Anticancer agent 50

Anticancer agent 50 (compound 6), a potent modulator of the ABCB1 efflux pump, exhibits cytotoxic and anti-proliferative activity by reducing cyclin D1 expression and inducing p53 expression. It shows significant potential for research in T lymphoma.

PF-2771 is a potent and selective centromere protein E (CENP-E) inhibitor with an IC50 of 16.1 nM, used as an anticancer agent.

Anticancer agent 38 (compound 19) is an aryl-urea compound, and is a potent anticancer agent. Anticancer agent 38 inhibits A431 cell growth with an IC 50 of 5.2 μg mL [1].

Tubulin Polymerization-IN-2 is a powerful anticancer agent that targets β-tubulin, exhibiting an IC 50 of 0.92 μM. It demonstrates promising efficacy against a range of cancer cell lines including leukemia, non-small cell lung, renal, prostate, and breast cancers [1].

Anticancer agent 37 (compound 18) is a sulfonylurea derivative known for its potent anticancer activity. It efficiently inhibits the growth of HePG2 cells, displaying an IC 50 value of 17.2 μg mL [1].

Anticancer agent 57 (compound 14) demonstrates potent inhibition of MDA-MB-231, MDA-MB-468, and MCF-7 cell lines, with IC50 values ranging from 6.43 to 8.00 μM. Additionally, this agent induces cell cycle arrest and promotes apoptosis. In vivo studies using nude mice xenografted with MADMB-231 cells have shown that Anticancer agent 57 effectively inhibits tumor growth. Consequently, Anticancer agent 57 can serve as a valuable tool for researching triple negative breast cancer (TNBC) [1].

Anticancer agent 35 (compound 10), a sulfonylurea derivative, is a potent anticancer agent that inhibits A549, A431, and PACA2 cell growth with IC50 values of 18.1 μg mL, 4.0 μg mL, and 18.9 μg mL, respectively [1].

Anticancer agent 63 (compound 3h) exhibits significant cytotoxic activity against multiple cancer cell lines, including SW480, HeLa, A549, and MCF-7, with IC50 values of 4.9, 11.5, 9.4, and 3.4 μM, respectively, after 24 hours of treatment. It induces apoptosis in MCF-7 cells by down-regulating Bcl-2 expression and up-regulating IL-2 and Caspase-3 expression, and also demonstrates antioxidative properties [1].

Anticancer agent 28 showed good anti-tumour effects in vivo in H22 allograft mice. anticancer agent 28 was 50 times more potent than Oridonin against K562 cells with an IC50 value of 0.09 μM.

Anticancer agent 25 demonstrates the highest level of cytotoxic effectiveness on PC3 cells, achieving an IC 50 value of 0.19 μM.

Anticancer agent 59, an inhibitor active against various cancer cell lines, particularly demonstrates efficacy in A549 cells with an IC 50 value of 0.2 μM. It prompts apoptosis, elevates Ca2+ and ROS levels within cancer cells, and markedly reduces mitochondrial membrane potential. Additionally, it effectively curtails tumor growth in the A549 mouse xenograft model.

4-Formylcolchicine, a potent anticancer agent, demonstrates cytotoxicity with IC 50 values of 1.007 µM for A549 cells, 0.128 µM for HT-29 cells, and 0.054 µM for HCT116 cells.

Gly-7-MAD-MDCPT is an anticancer agent. Gly-7-MAD-MDCPT is a Camptothecin compound, it shows cytotoxicity to various cancer cells with IC 50 values of 10-1000 nM [1] .

Aviculin, a lignan glycoside, exhibits significant anticancer properties, particularly in inhibiting the metabolic activity of MCF-7 cells to below 50%, with an IC 50 value of 75.47 μM. It promotes apoptosis in breast cancer cells via the intrinsic apoptosis pathway, enhancing the expression of initiator caspase-9, executioner caspase-7, and poly (ADP-ribose) polymerase (PARP). Furthermore, Aviculin leads to an increased Bax Bcl-2 ratio, underlying its potential as an effective anticancer agent.

Compound 6, fac-[Re(CO)3(L6)(H2O)][NO3], a rhenium(I) tricarbonyl aqua complex, serves as an anticancer agent by disrupting mitochondrial function. It exhibits cytotoxicity against prostate cancer cells with an IC50 of 50 nM in PC-3 cells. This compound predominantly localizes in the nucleus, impairs ATP production, and induces apoptosis in PC3 cells without causing necrosis, pyroptosis, or autophagy [1].

Antitumor agent-107 (compound 5h) is an anticancer agent exhibiting potent inhibitory activity against leukemia cell lines (GI50 = 0.32-1.34 μM) and demonstrating broad-spectrum antitumor effects across various human cancer cell lines (GI50 = 0.35-9.43 μM) [1].

Azurin (50-77) is a peptide fragment derived from the copper-containing bacterial protein azurin, present in P. aeruginosa. It exhibits properties that regulate the cell cycle, inhibit cancer proliferation, and manage angiogenesis, proving its potential as an anticancer agent. Specifically, this compound acts as a VEGFR2 inhibitor with an IC20 of approximately 10.7 µM. At a concentration of 20 µM, it effectively induces cell cycle arrest at the G2 M phase in MCF-7 breast cancer cells, while a higher concentration of 50 µM significantly reduces the proliferation of both MCF-7 and ZR-75-1 breast cancer cell lines. Furthermore, Azurin (50-77) impedes VEGF-A-induced capillary tube formation with an IC50 of 12 µM, and alters the cellular and extracellular levels of critical signaling and structural proteins such as F-actin, focal adhesion kinase (FAK), paxillin, and platelet endothelial cell adhesion molecule-1 (PECAM-1) in human umbilical vein endothelial cells (HUVECs) at a concentration of 25 µM. Demonstrating its efficacy in vivo, Azurin (50-77) administered at 10 mg kg per day notably reduces tumor volume in an MCF-7 mouse xenograft model, highlighting its therapeutic potential.

8-Chloroadenosine-5'-triphosphate (8-chloro ATP), a potent metabolite of the anticancer agent 8-chloro cyclic AMP (cAMP) and a nucleotide derivative, is produced through the biotransformation of 8-chloro cAMP into 8-chloroadenosine, followed by mono- and diphosphate intermediates. Accumulating for up to 12 hours after the administration of 8-chloro cAMP or 8-chloroadenosine, 8-chloro ATP inhibits cell growth, diminishes endogenous ATP levels, and reduces RNA synthesis without affecting DNA synthesis in multiple myeloma cells derived from patients. Moreover, it obstructs topoisomerase II-α-mediated relaxation of supercoiled pUC19 DNA at concentrations ranging from 1.5 to 8 mM and decreases topoisomerase II-α-enhanced ATP hydrolysis by 50% at a concentration of 1 mM in K562 human myelocytic leukemia cells.

Antitumor agent-144 (16) functions as an anticancer compound, exhibiting IC 50 values of 2.6 μM in L1210 cells and 8.4 μM in KB cells, respectively [1].

Isolicoflavonol is a potential cancer chemopreventive agent.

Isofuranodiene protects GalN LPS-induced liver injury in SD rats, it may be a potential functional food ingredient for the prevention and treatment of liver diseases. Isofuranodiene has anticancer activity, by inhibiting the proliferation and inducing apo