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DNA/RNA Synthesis inhibitor
Tegafur is a chemotherapeutic 5-FU prodrug used in the treatment of cancers. It is a component of tegafur-uracil.- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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viral RNA polymerase inhibitor
T-705, a substituted pyrazine compound, has been found to exhibit potent anti-influenza virus activity in vitro and in vivo.
- Thomas R Lane, .et al. , ACS Infect Dis, 2026, May 8;12(5):1776-1789 PMID: 42052926
- Dylan M Johnson, .et al. , Viruses, 2024, Jul 9;16(7):1101 PMID: 39066263
- Steven B Tillis, .et al. , Microorganisms, 2023, May 24;11(6):1371 PMID: 37374873
- Hyeon-Min Cha, .et al. , ACS Infect Dis, 2023, Apr 14;9(4):1033-1045 PMID: 36912867
- Satoko Yamaoka, .et al. , Antiviral Res, 2022, Apr;200:105291 PMID: 35296419
- Crystal A Mendoza, .et al. , Antiviral Res, 2021, Jan;185:104993 PMID: 33296695
- Liva Checkmahomed, .et al. , Viruses, 2020, Oct; 12(10): 1139 PMID: 33049959
- JE Comer, .et al. , Viruses, 2019, Feb 3;11(2). pii: E137 PMID: 30717492
- Ma J, .et al. , Antiviral Res, 2018, Feb;150:112-122 PMID: 29253498
- Ji-Ae Kim, .et al. , Viruses, 2018, Feb; 10(2): 72 PMID: 29425176
- Haejin Chun, .et al. , Polym Chem, 2018, 9: 2116-2123
- Baz M, .et al. , Viruses, 2018, Nov 3;10(11) PMID: 30400276
- Sehee Park, .et al. , PLoS One., 2014, 9(7): e101325 PMID: 24992479
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PARP inhibitor
PJ34 is a novel potent specific inhibitor of PARP-l/2 with EC50 of 20 nM.- Tim J Wigle, .et al. , Cell Chem Biol, 2020, Jul 16;27(7):877-887 PMID: 32679093
- 5-Fluorouridine is a metabolite of 5-fluorouracil with anticancer activity.
- Tz-Feng Lin, .et al. , Mater Today Commun, 2022, 33: 104284
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Topoisomerase inhibitor
Amonafide is a DNA intercalator and topoisomerase II inhibitor for the treatment of neoplastic diseases, one of Antitumor agent.
- Veronica Rendo, .et al. , Nat Commun, 2020, 11: 1308 PMID: 32161261
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HDAC3 inhibitor
RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM, exhibits > 200-fold selectivity over other HDAC.- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
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Topoisomerase IV inhibitor
Ciprofloxacin Hydrochloride is a broad-spectrum antimicrobial carboxyfluoroquinoline, interfering with the bacterial DNA gyrase, inhibiting the DNA synthesis, and preventing bacterial cell growth.- Viktoria Lazar, .et al. , Nature, 2022, 610: 540-546 PMID: 36198788
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PARP1 inhibitor
AG14361 is a potent PARP inhibitor, enhanced TMZ cytotoxicity in MMR(mismatch repair)-proficient / deficient cells.- Vimal Pandey, .et al. , Scientific Reports, 2019, 9, Article number: 5012 PMID: 30899038
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Topoisomerase inhibitor
Idarubicin is an anthracycline antibiotic that is an anti-leukemia agent with higher DNA binding capacity and greater cytotoxicity than daunorubicin.- Wei Y, .et al. , Mol Cell, 2017, Jun 1;66(5):581-596.e6 PMID: 28552615
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PI3K inhibitor
Wortmannin is a potent, selective, cell-permeable and irreversible inhibitor of phosphatidylinositol 3-kinase (PI 3-kinase) (IC50 = 2 - 4 nM) which also potently inhibits polo-like kinase 1 (PLK1) (IC50 = 5.8 nM).
- Weili Chen, .et al. , Communications Biology, 2024, 7:488 PMID: 38649462
- Hirotake Ishida, .et al. , J Neurosci, 2021, Oct 13;41(41):8494-8507 PMID: 34452938
- Actinomycin D is a metabolite isolated from Streptomyces parvulus that binds to the GpC steps of DNA. The compound acts as an antibiotic and is more effective against gram-positive bacteria than gram negative bacteria.
- Wenjia Xia, .et al. , J RADIAT RES APPL SC, 2026, 19: 102504
- Jiayuan Hu, .et al. , Cancer Metab, 2025, Jun 18;13(1):32 PMID: 40533864
- Danjun Wang, .et al. , Applied Biological Chemistry, 2025, 68: 24
- Hongbo Liu, .et al. , Cancer Biol Ther, 2025, Dec;26(1):2479926 PMID: 40176374
- Lixia Wu, .et al. , J Transl Med, 2025, Apr 1;23(1):385 PMID: 40170133
- Akane Ogawa, .et al. , Mol Cell, 2025, Mar 6;85(5):894-912 PMID: 39909041
- Ruo-Yang Chen, .et al. , International Immunopharmacology, 2025, 147: 113920 PMID: 39799734
- Zegui N, .et al. , Cancer Research, 2022, FEBRUARY 22 PMID: 35502544
- Lina Gu, .et al. , Molecular Cancer, 2022, 21:217 PMID: 36514094
- Chauhan D, .et al. , Cell Rep, 2018, Nov 27;25(9):2354-2368.e5 PMID: 30485805
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PARP inhibitor
PJ 34 hydrochloride is a potent inhibitor of poly(ADP-ribose) polymerase (PARP) (EC50 = 20 nM).- Wigle TJ, .et al. , SLAS Discov, 2019, Dec 19:2472555219883623 PMID: 31855104
- Alvin Z.Lu, .et al. , Biochem Pharmacol, 2019, May 7. pii: S0006-2952(19)30171-6 PMID: 31075269
- Hoechst 33258 trihydrochloride is a cell dye for DNA quantitation.
- Xiao-Hong Guo, .et al. , Oncol Rep, 2021, Dec;46(6):253 PMID: 34643248
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DNA topoisomerase II inhibitor
Beta-Lapachone is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase.- Xiaoling Li, .et al. , ACS Appl. Bio Mater, 2020, 3, 3, 1769-1778 PMID: 35021666
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DNA/RNA Synthesis inhibitor
Clofarabine is a second generation purine nucleoside analog with antineoplastic activity- Xie J, .et al. , Pediatr Blood Cancer, 2019, Dec 25:e28133 PMID: 31876116
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Topoisomerase inhibitor
Epirubicin is a cell-permeable antitumor antibiotic. A stereoisomer of Doxorubicin that exhibits reduced cardiotoxicity. Epirubicin?€?s antitumor actions are mediated by targeting and inhibiting Topo II (topoisomerase II).- Xiu-wu Pan, .et al. , Oncol Rep, 2016, Jan;35(1):334-42 PMID: 26496799
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Selective SIRT2 inhibitor
SirReal2 is a potent and selective Sirt2 inhibitor with IC50 of 140 nM.- Yang Li, .et al. , Neoplasia, 2018, Jul; 20(7): 745-756 PMID: 29925042
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DNA/RNA Synthesis inhibitor
Oxaliplatin is a platinum-based antineoplastic agent that is used in cancer chemotherapy. In vivo studies showed that Oxaliplatin has anti-tumor activity against colon carcinoma through its (non-targeted) cytotoxic effects.- Yao-Yu Hsieh, .et al. , Mol Oncol, 2023, Oct 16 PMID: 37842807
- Mohamed Elbadawy, .et al. , Biomed Pharmacother, 2021, Oct;142:112043 PMID: 34411919
- Tatsuya Usui, .et al. , Int J Mol Sci, 2018, Apr; 19(4): 1098 PMID: 29642386
- Shimokawa M, .et al. , Nature, 2017, May 11;545(7653):187-192 PMID: 28355176
- Eri Takiguchi, .et al. , Exp Ther Med, 2017, Nov; 14(5): 4293-4299 PMID: 29067110
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ATM/ATR inhibitor
VE-821 is a potent and selective inhibitor of protein kinase ATR.- Yiovana Veronica Okraine, .et al. , Cell Death Dis, 2025, Jul 8;16(1):503 PMID: 40628724
- Atsushi Saito, .et al. , Cell Rep, 2023, May 30;42(5):112479 PMID: 37178686
- Mitsuru Sasaki-Honda, .et al. , Hum Mol Genet, 2018, Dec 1; 27(23): 4024-4035 PMID: 30107443
- Kim J, .et al. , Mol Cell, 2018, Jan 4;69(1):36-47.e7 PMID: 29249653
- Antonio Postigo, .et al. , Cell Rep, 2017, May 2; 19(5): 1022-1032 PMID: 28467896
- Nnennaya Kanu, .et al. , Genome Biol, 2016, 17: 185 PMID: 27634334
- Carolyn Botting, .et al. , Virol J, 2016, 13: 15 PMID: 26817608
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HDAC inhibitor
TMP 269 is a potent, selective class IIa HDAC inhibitor with IC50 of 157 nM, 97 nM, 43 nM and 23 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.- Yodita Asfaha, .et al. , Eur J Med Chem, 2024, 263: 115907 PMID: 37979441
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HDAC inhibitor
AR-42 is a novel HDAC inhibitor, exhibits biologic activity against malignant mast cell lines via down-regulation of constitutively activated Kit.- Yong-Hui Liao, .et al. , Mol Med Rep, 2018, Feb; 17(2): 2803-2810 PMID: 29257262
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DNA/RNA Synthesis inhibitor
Raltitrexed (Tomudex) is an inhibitor of thymidylate synthase and also is one of the strongest antimetabolites in use.- Yool Lee, .et al. , Sci Adv, 2021, 7 PMID: 33579708
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PARP inhibitor
Olaparib (AZD2281) is an inhibitor of poly ADP ribose polymerase (PARP), an enzyme involved in DNA repair.- Yuki Yoshino, .et al. , Biochem Biophys Res Commun, 2025, Jan:742:151153 PMID: 39672008
- Saptarshi Sinha, .et al. , Med Oncol, 2024, Jan 6;41(2):49 PMID: 38184505
- Erika Nakatsuka, .et al. , Transl Oncol, 2024, Sep 12:50:102119 PMID: 39270525
- Callum G Jones, .et al. , Cancers (Basel), 2024, Feb 21;16(5):863 PMID: 38473223
- Aurelie Vanderlinden, .et al. , Br J Cancer, 2023, Nov;129(11):1829-1840 PMID: 37777579
- Saptarshi Sinha, .et al. , Exp Cell Res, 2022, Nov 1;420(1):113338 PMID: 36075449
- Subhajit Chatterjee, .et al. , J Cancer Res Clin Oncol, 2022, Dec;148(12):3521-3535 PMID: 35962813
- Yuki Uchihara, .et al. , Mol Cell, 2022, Jul 21;82(14):2557-2570 PMID: 35594857
- Ji-Ye Kim, .et al. , Cell Death Dis, 2022, Mar 15;13(3):239 PMID: 35293383
- Emad Matanes, .et al. , Front Oncol, 2021, Oct 27;11:745981 PMID: 34778062
- Shino Endo, .et al. , Cancer Res Commun, 2021, 1(2): 90-105 PMID: 36860287
- Yan Baglo, .et al. , Transl Oncol, 2021, Nov;14(11):101198 PMID: 34418731
- Joseph M Gozgit, .et al. , Cancer cell, 2021, Jul 22;S1535-6108(21)00340-8 PMID: 34375612
- Sefinew Molla, .et al. , DNA Repair (Amst), 2021, Jun 10;105:103157 PMID: 34144488
- Jianming Wang, .et al. , Cell Rep, 2021, Feb 16;34(7):108759 PMID: 33596418
- Ai Ito, .et al. , Biogerontology, 2021, Feb;22(1):119-131 PMID: 33216250
- Tim J Wigle, .et al. , Cell Chem Biol, 2020, Jul 16;27(7):877-887 PMID: 32679093
- Ali Divan, .et al. , Pharmacol Res Perspect, 2020, Apr; 8(2): e00586 PMID: 32342655
- Jianwei Dou, .et al. , J Sep Sci, 2020, Dec 4 PMID: 33275824
- Sai Dimple Manavitha Gullipalli, .et al. , Int. J. Adv. Pharm. Biotech, 2020, 6(2) 01-08
- Chao Zhang, .et al. , J Atheroscler Thromb, 2020, Sep 25 PMID: 32981917
- Wigle TJ, .et al. , SLAS Discov, 2019, Dec 19:2472555219883623 PMID: 31855104
- Wang Q, .et al. , Cancer Med, 2019, Dec 21 PMID: 31863638
- Molla S, .et al. , Pathol Oncol Res, 2019, Nov 25 PMID: 31768967
- Alvin Z.Lu, .et al. , Biochem Pharmacol, 2019, May 7. pii: S0006-2952(19)30171-6 PMID: 31075269
- Bian C, .et al. , Nat Commun, 2019, Feb 11;10(1):693 PMID: 30741937
- HC de Silva, .et al. , Cell Mol Life Sci, 2019, 1-16 PMID: 30725116
- Kamada Y, .et al. , Fitoterapia, 2018, Sep;129:94-101 PMID: 29928967
- 2018, .et al. , FEBS Open Bio, 2018, Jun; 8(6): 1001-1012 PMID: 29928579
- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Hiro Sato, .et al. , Nat Commun, 2017, 8: 1751 PMID: 29170499
- Charles-André Philip, .et al. , BMC Cancer, 2017, 17: 638 PMID: 28886696
- Rulina AV, .et al. , Cell Death Dis, 2016, Dec 1;7(12):e2505 PMID: 27906189
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DNA synthesis inhibitor
Mitomycin C is a DNA crosslinking agent that inhibits DNA synthesis and induces apoptosis in a variety of cells.- Zhang H, .et al. , Cancer Commun, 2026, 46:Article 0028 PMID: 42147354
- Clement J F Heymann, .et al. , Res Sq, 2025, Nov 24:rs.3.rs-8051355 PMID: 41356367
- John A. Quinlan, .et al. , Advanced Nano Biomed, 2024, Sep 28 PMID: 41551720
- Gehlen-Breitbach S, .et al. , Int J Oral Sci, 2023, 15(1):16 PMID: 37024457
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DDX3 inhibitor
RK-33 is a potent and selective DDX3 inhibitor. RK-33 binds to DDX3 and abrogates its activity.- Zhang S, .et al. , Sci Rep, 2020, Jan 31;10(1):1557 PMID: 32005838
- Yang SNY, .et al. , Cells, 2020, Jan 9;9(1). PMID: 31936642
- NKP-1339 (IT-139) is the first-in-class ruthenium-based anticancer drug in clinical development against solid cancer with limited side effects.
- Zin Zin Ei, .et al. , Sci Rep, 2021, Nov 17;11(1):22448 PMID: 34789798
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Transcriptase inhibitor
Abacavir sulfate is a nucleoside analog reverse transcriptase inhibitor (NRTI); guanosine analog used to treat HIV and AIDS. -
MDMX Inhibitor
NSC207895 is a cell-permeable benzofuroxan compound that downregulates the p53 negative regulator MDMX protein level in MCF-7, LNCaP, and A549 cells (1 to 10 µM for 16 to 24 h) by suppressesing MDMX promoter transcription activity (IC50 = 2.5 µM in HT1080 cells), leading to enhanced p53 stabilization and activation.
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Polymerase inhibitor
Balapiravir (R1626, RG1626) is the prodrug of a nucleoside analogue inhibitor of the hepatitis C virus (HCV) RNA-dependent RNA polymerase (R1479, RG1479). -
DHFR inhibitor
Pralatrexate is an antifolate (a folate analogue metabolic inhibitor) designed to accumulate preferentially in cancer cells. -
HCV NS5B polymerase inhibitor
Mericitabine (RG 7128; R-7128) is a nucleoside inhibitor of the HCV NS5B polymerase that acts as an RNA chain terminator and prevents elongation of RNA transcripts during replication. -
eIF4A inhibitor
Silvestrol is a eukaryotic translation initiation factor 4A (eIF4A) inhibitor isolated from the fruits and twigs of Aglaia foveolata. Silvestrol induces autophagy and caspase-mediated apoptosis. - Silvestrol aglycone is a Silvestrol analogue, inhibits protein translation initiation in cancer cells, with EC50s of 10 and 200 nM for myc-LUC and tub-LUC luciferase reporter protein translation, respectively. Anti-cancer activity.
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NS5B polymerase inhibitor
Tegobuvir (GS-9190 is a non-nucleoside NS5B polymerase inhibitor. - Triptolide is a diterpene triepoxide, immunosuppresive agent extracted from the Chinese herb Tripterygium wilfordii.
- Levoleucovorin calcium is the calcium salt of Levoleucovorin, which is the enantiomerically active form of folinic acid.
- Procarbazine Hydrochloride is an alkylating agent, with anticancer activity.
- Cyclophosphamide monohydrate is an alkylating, cytotoxic agent experimentally shown to crosslink DNA, causing strand breakage and inducing mutations.
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Topoisomerase inhibitor
Balofloxacin is a quinolone antibiotic. The bactericidal action of Balofloxacin results from interference with the enqyme DNA gyrase which is needed for the synthesis of bacterial DNA. Balofloxacin is efficacious against Gram-negative bacteria. It also has enhanced activity against Gram positive bacteria, including MRSA and Streptococcus pneumoniae. -
Topoisomerase inhibitor
Sarafloxacin hydrochloride is a fluoroquinolone antibacterial agent. Inhibits bacterial DNA gyrase (topoisomerase).

