a2780 cells

Oxaliplatin (L-OHP) is a DNA alkylating agent, an inhibitor of DNA synthesis. Oxaliplatin causes DNA cross-linking damage, preventing DNA replication and transcription and leading to cell death. Oxaliplatin induces autophagy.

Bortezomib (LDP 341) is a 20S proteasome inhibitor (Ki=0.6 nM) that is reversible and selective. Bortezomib has antitumor activity and inhibits NF-κB, which can disrupt the cell cycle and induce apoptosis.

Deferoxamine (Desferrioxamine B) is an iron chelator. Deferoxamine can be used to reduce the accumulation and deposition of iron in tissues. Deferoxamine can improve neurological dysfunction by inhibiting ferroptosis and neuroinflammation after traumatic brain injury. It has antioxidant, anti-proliferation and anti-tumor activities, and can induce the production of HIF-1α, apoptosis and autophagy in cancer cells. It can be used to treat acute iron toxicity and COVID-19 related diseases.

Vorinostat (SAHA) is a pan-histone deacetylase (HDAC) inhibitor (IC50=10 nM) with inhibitory activity against HDAC1/2/3/6/7/11. Vorinostat has antitumor activity, induces cell differentiation, blocks the cell cycle and induces apoptosis.

Dorsomorphin (BML-275) is an AMPK inhibitor (Ki=109 nM) that is selective and ATP-competitive. Dorsomorphin inhibits the BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy, and possesses antitumor activity.

Tamoxifen is an orally active selective estrogen receptor modulator (SERM) that acts as an estrogen antagonist in breast cells and an agonist in bone, liver, and uterine cells. It can be used to induce gene knockout and liver injury models in mice, and also exhibits multiple biological activities, including activation of Hsp90, induction of autophagy and apoptosis, and inhibition of EBOV and MARV viral infections.

Etoposide (VP-16-213) is a topoisomerase II inhibitor that inhibits DNA synthesis by forming a complex with topoisomerase II and DNA (IC50=60.3 μM). Etoposide has antitumor activity and induces apoptosis and autophagy.

Carboplatin (JM-8) is a cisplatin derivative, a DNA synthesis inhibitor. Carboplatin binds to DNA, inhibits replication and transcription, and induces cell death. Carboplatin has antitumor activity.

Daphnetin (7,8-Dihydroxycoumarin), a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities.

Irinotecan (CPT-11), a derivative of camptothecin, is an inhibitor of DNA topoisomerase I (Topo I). Irinotecan has antitumor activity by preventing DNA strand reattachment through binding to the Topo I complex, resulting in double-stranded DNA breaks and cell death.

Imatinib (STI571) is a multi-targeted receptor tyrosine kinase inhibitor that selectively inhibits the kinase activities of BCR/ABL, v-Abl, PDGFR, and c-kit with oral activity. Imatinib has antitumor activity for the treatment of chronic granulocytic leukemia.

Mitoxantrone (mitozantrone) is an anthracenedione antibiotic with antineoplastic activity. Mitoxantrone intercalates into and crosslinks DNA, thereby disrupting DNA and RNA replication. This agent also binds to topoisomerase II, resulting in DNA strand breaks and inhibition of DNA repair. Mitoxantrone is less cardiotoxic compared to doxorubicin.

2-Methylcyclohexa-2,5-diene-1,4-dione exhibits inhibitory activity against cancer cells such as A2780, HT-29, HL-60, and K562 (IC50 = 2.8–12.1 µM) and antibacterial activity against Bacillus subtilis.

P-gp inhibitor 27 (Compound D2) is an inhibitor of P-glycoprotein (P-gp) that reduces the expression of P-gp and MRP1. It increases the accumulation of Rh123 in A2780 T cells and reverses multidrug resistance to Paclitaxel (EC50 of 88 nM) and Cisplatin.

DS-103 is an HDAC inhibitor that targets HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 with IC50 values of 0.029, 0.123, 0.022, 0.367, and 9.26 μM, respectively. It also inhibits the malignant malaria parasite [Plasmodium falciparum 3D7] with an IC50 of 5.08 μM. In A2780 and Cal27 cells, DS-103 exhibits cytotoxicity with IC50 values of 1.48 μM and 1.47 μM, respectively, and reverses cisplatin resistance in these cells with IC50 values of 4.62 μM and 2.23 μM. DS-103 acts synergistically with cisplatin, enhancing apoptosis induced by cisplatin.

BMS-265246 is a potent and selective CDK1 2 inhibitor. Its chemical name is (4-[R-(2,3-Dihydro-benzo[1,4]dioxin-6-yl)-1H-indol-1-yl]-1H-pyrazolo[3,4-d] pyrimidine-6-amine), and it functions by targeting CDK1 and CDK2 to potentially disrupt cell cycle progression.

10'-Desmethoxystreptonigrin is an antibiotic originally isolated from Streptomyces and a derivative of the antibiotic streptonigrin. It is active against a variety of bacteria, including S. aureus, S. faecalis, E. coli, K. pneumoniae, and P. vulgaris (MICs = 0.4, 1.6, 3.1, 3.1 and 0.4 μg/ml, respectively). 10'-Desmethoxystreptonigrin is cytotoxic to HCT116 colon and A2780 ovarian cancer cells (IC50s = 0.004 and 0.001 μg/ml, respectively), as well as HCT116 cells resistant to etoposide and teniposide and cisplatin-resistant A2780 cells (IC50s = 0.003, 0.001, and 0.01 μg/ml, respectively). 10'-Desmethoxystreptonigrin is also an inhibitor of p21ras farnesylation (IC50 = 21 nM).

4-oxo-27-TBDMS Withaferin A is a derivative of the steroidal lactone withaferin A that has anticancer activity.1 It is cytotoxic to A2780 ovarian cancer cells (IC50 = 17 μM) but not to carboplatin-resistant A2780 (A2780/CP70) cells (IC50 = >100 μM). It is selective for A2780 cells over non-cancerous ARPE19 cells (IC50 = 1,660 μM). 4-oxo-27-TBDMS Withaferin A induces DNA fragmentation in A2780 cells.References1. Perestelo, N.R., Llanos, G.G., Reyes, C.P., et al. Expanding the chemical space of withaferin A by incorporating silicon to improve its clinical potential on human ovarian carcinoma cells. J. Med. Chem. 62(9), 4571-4585 (2019). 4-oxo-27-TBDMS Withaferin A is a derivative of the steroidal lactone withaferin A that has anticancer activity.1 It is cytotoxic to A2780 ovarian cancer cells (IC50 = 17 μM) but not to carboplatin-resistant A2780 (A2780/CP70) cells (IC50 = >100 μM). It is selective for A2780 cells over non-cancerous ARPE19 cells (IC50 = 1,660 μM). 4-oxo-27-TBDMS Withaferin A induces DNA fragmentation in A2780 cells. References1. Perestelo, N.R., Llanos, G.G., Reyes, C.P., et al. Expanding the chemical space of withaferin A by incorporating silicon to improve its clinical potential on human ovarian carcinoma cells. J. Med. Chem. 62(9), 4571-4585 (2019).

Thymohydroquinone (Thymoquinol) is a monoterpenoid phenolic compound found in thyme, oregano, and other plants in the labiaceae family. Thymohydroquinone inhibits cancer cell growth, reduces oxidative stress and modulates inflammatory responses, scoured 2, 2-diphenyl-1-PicrylHydrazyl radicals in a cell-free assay (IC50 = 2.4 μg ml), In the oxygen radical absorption capacity (ORAC) test at concentrations of 1.6 to 6.4 μg ml, Its Trolox value was 2.6. Thymus hydroquinone inhibited the growth of A2780, OVCAR-8 and CIS-A2780 ovarian cancer cells (IC50 were 3.1, 8.9 and 9.8 μM, respectively) and human ovarian immortalized epithelial cells (IC50 = 14 μM). It also inhibited Plasmodium falciparum in vitro (IC50 = 15.9 μM).

4-oxo Withaferin A is a derivative of the steroidal lactone withaferin A that has anticancer activity.1 It is cytotoxic to A2780 ovarian cancer cells and carboplatin-resistant A2780 (A2780/CP70) cells (IC50s = 7.3 and <1 μM, respectively) and is 4.4-fold selective for A2780 cells over non-cancerous ARPE19 cells.References1. Perestelo, N.R., Llanos, G.G., Reyes, C.P., et al. Expanding the chemical space of withaferin A by incorporating silicon to improve its clinical potential on human ovarian carcinoma cells. J. Med. Chem. 62(9), 4571-4585 (2019). 4-oxo Withaferin A is a derivative of the steroidal lactone withaferin A that has anticancer activity.1 It is cytotoxic to A2780 ovarian cancer cells and carboplatin-resistant A2780 (A2780/CP70) cells (IC50s = 7.3 and <1 μM, respectively) and is 4.4-fold selective for A2780 cells over non-cancerous ARPE19 cells. References1. Perestelo, N.R., Llanos, G.G., Reyes, C.P., et al. Expanding the chemical space of withaferin A by incorporating silicon to improve its clinical potential on human ovarian carcinoma cells. J. Med. Chem. 62(9), 4571-4585 (2019).

Liriopesides B (Nolinospiroside F) exhibited potential anticancer activity against human ovarian cancer A2780 cells.

Trifolirhizin exerts varying degrees of inhibition on tyrosinase-dependent melanin biosynthesis, and therefore, are candidates as skin-whitening agents.Trifolirhizin possesses potential anti-inflammatory and anti-cancer activities.Trifolirhizin shows in vitro inhibitory effects on the growth of human A2780 ovarian and H23 lung cancer cells. Trifolirhizin inhibits acetylcholine mediated airway smooth muscle (ASM) contraction or directly relaxes pre-contracted ASM independent of β 2 -adrenoceptors.

Nutlin-3a is the active enantiomer of Nutlin-3, an MDM2 antagonist that inhibits MDM2-p53 interaction (Ki=90 nM) and activates p53. Nutlin-3a binds preferentially to the p53-binding pocket of MDM2, leading to stabilization of p53 and activation of the p53 pathway. Nutlin-3a has antitumor activity.

Dorsomorphin dihydrochloride (BML-275 2HCl) is a potent, selective and ATP-competitive AMPK inhibitor (Ki: 109 nM) and does not exhibit significant activity on structurally related kinases.