BIOMAT Database Logo BIOMAT Database Logo

Novel Chrysin-De-Allyl PAC-1 Hybrid Analogues as Anticancer Compounds: Design, Synthesis, and Biological Evaluation. 2020

Buthina A Al-Oudat, and Hariteja Ramapuram, and Saloni Malla, and Suaad A Audat, and Noor Hussein, and Jenna M Len, and Shikha Kumari, and Mel F Bedi, and Charles R Ashby, and Amit K Tiwari
Department of Medicinal Chemistry and Pharmacognosy, Faculty of Pharmacy, Jordan University of Science and Technology, P.O. Box 3030, Irbid 22110, Jordan.

New chrysin-De-allyl-Pac-1 hybrid analogues, tethered with variable heterocyclic systems (4a-4o), were rationally designed and synthesized. The target compounds were screened for in vitro antiproliferative efficacy in the triple-negative breast cancer (TNBC) cell line, MDA-MB-231, and normal human mammary epithelial cells (HMECs). Two compounds, 4g and 4i, had the highest efficacy and selectivity towards MDA-MB-231 cells, and thus, were further evaluated by mechanistic experiments. The results indicated that both compounds 4g and 4i induced apoptosis by (1) inducing cell cycle arrest at the G2 phase in MDA-MB-231 cells, and (2) activating the intrinsic apoptotic pathways in a concentration-dependent manner. Physicochemical characterizations of these compounds suggested that they can be further optimized as potential anticancer compounds for TNBC cells. Overall, our results suggest that 4g and 4i could be suitable leads for developing novel compounds to treat TNBC.

UI MeSH Term Description Entries
D010879 Piperazines Compounds that are derived from PIPERAZINE.
D002453 Cell Cycle The complex series of phenomena, occurring between the end of one CELL DIVISION and the end of the next, by which cellular material is duplicated and then divided between two daughter cells. The cell cycle includes INTERPHASE, which includes G0 PHASE; G1 PHASE; S PHASE; and G2 PHASE, and CELL DIVISION PHASE. Cell Division Cycle,Cell Cycles,Cell Division Cycles,Cycle, Cell,Cycle, Cell Division,Cycles, Cell,Cycles, Cell Division,Division Cycle, Cell,Division Cycles, Cell
D002465 Cell Movement The movement of cells from one location to another. Distinguish from CYTOKINESIS which is the process of dividing the CYTOPLASM of a cell. Cell Migration,Locomotion, Cell,Migration, Cell,Motility, Cell,Movement, Cell,Cell Locomotion,Cell Motility,Cell Movements,Movements, Cell
D005260 Female Females
D005419 Flavonoids A group of phenyl benzopyrans named for having structures like FLAVONES. 2-Phenyl-Benzopyran,2-Phenyl-Chromene,Bioflavonoid,Bioflavonoids,Flavonoid,2-Phenyl-Benzopyrans,2-Phenyl-Chromenes,2 Phenyl Benzopyran,2 Phenyl Benzopyrans,2 Phenyl Chromene,2 Phenyl Chromenes
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D006835 Hydrazones Compounds of the general formula R:N.NR2, as resulting from the action of hydrazines with aldehydes or ketones. (Grant & Hackh's Chemical Dictionary, 5th ed) Hydrazone
D000498 Allyl Compounds Alkenes with the general formula H2C Compounds, Allyl
D000970 Antineoplastic Agents Substances that inhibit or prevent the proliferation of NEOPLASMS. Anticancer Agent,Antineoplastic,Antineoplastic Agent,Antineoplastic Drug,Antitumor Agent,Antitumor Drug,Cancer Chemotherapy Agent,Cancer Chemotherapy Drug,Anticancer Agents,Antineoplastic Drugs,Antineoplastics,Antitumor Agents,Antitumor Drugs,Cancer Chemotherapy Agents,Cancer Chemotherapy Drugs,Chemotherapeutic Anticancer Agents,Chemotherapeutic Anticancer Drug,Agent, Anticancer,Agent, Antineoplastic,Agent, Antitumor,Agent, Cancer Chemotherapy,Agents, Anticancer,Agents, Antineoplastic,Agents, Antitumor,Agents, Cancer Chemotherapy,Agents, Chemotherapeutic Anticancer,Chemotherapy Agent, Cancer,Chemotherapy Agents, Cancer,Chemotherapy Drug, Cancer,Chemotherapy Drugs, Cancer,Drug, Antineoplastic,Drug, Antitumor,Drug, Cancer Chemotherapy,Drug, Chemotherapeutic Anticancer,Drugs, Antineoplastic,Drugs, Antitumor,Drugs, Cancer Chemotherapy
D014407 Tumor Cells, Cultured Cells grown in vitro from neoplastic tissue. If they can be established as a TUMOR CELL LINE, they can be propagated in cell culture indefinitely. Cultured Tumor Cells,Neoplastic Cells, Cultured,Cultured Neoplastic Cells,Cell, Cultured Neoplastic,Cell, Cultured Tumor,Cells, Cultured Neoplastic,Cells, Cultured Tumor,Cultured Neoplastic Cell,Cultured Tumor Cell,Neoplastic Cell, Cultured,Tumor Cell, Cultured

Related Publications

Buthina A Al-Oudat, and Hariteja Ramapuram, and Saloni Malla, and Suaad A Audat, and Noor Hussein, and Jenna M Len, and Shikha Kumari, and Mel F Bedi, and Charles R Ashby, and Amit K Tiwari
Design, synthesis and biological evaluation of chrysin benzimidazole derivatives as potential anticancer agents.
December 2018, Natural product research,
Buthina A Al-Oudat, and Hariteja Ramapuram, and Saloni Malla, and Suaad A Audat, and Noor Hussein, and Jenna M Len, and Shikha Kumari, and Mel F Bedi, and Charles R Ashby, and Amit K Tiwari
Design, synthesis and biological evaluation of arylcinnamide hybrid derivatives as novel anticancer agents.
June 2014, European journal of medicinal chemistry,
Buthina A Al-Oudat, and Hariteja Ramapuram, and Saloni Malla, and Suaad A Audat, and Noor Hussein, and Jenna M Len, and Shikha Kumari, and Mel F Bedi, and Charles R Ashby, and Amit K Tiwari
Design, synthesis and biological evaluation of chrysin long-chain derivatives as potential anticancer agents.
February 2010, Bioorganic & medicinal chemistry,
Buthina A Al-Oudat, and Hariteja Ramapuram, and Saloni Malla, and Suaad A Audat, and Noor Hussein, and Jenna M Len, and Shikha Kumari, and Mel F Bedi, and Charles R Ashby, and Amit K Tiwari
Design, synthesis and biological evaluation of novel indolin-2-ones as potent anticancer compounds.
August 2017, Bioorganic & medicinal chemistry letters,
Buthina A Al-Oudat, and Hariteja Ramapuram, and Saloni Malla, and Suaad A Audat, and Noor Hussein, and Jenna M Len, and Shikha Kumari, and Mel F Bedi, and Charles R Ashby, and Amit K Tiwari
Design, synthesis and biological evaluation of novel hybrid compounds of imidazole scaffold-based 2-benzylbenzofuran as potent anticancer agents.
April 2013, European journal of medicinal chemistry,
Buthina A Al-Oudat, and Hariteja Ramapuram, and Saloni Malla, and Suaad A Audat, and Noor Hussein, and Jenna M Len, and Shikha Kumari, and Mel F Bedi, and Charles R Ashby, and Amit K Tiwari
Synthesis and biological evaluation of novel C (7) modified chrysin analogues as antibacterial agents.
January 2006, Bioorganic & medicinal chemistry letters,
Buthina A Al-Oudat, and Hariteja Ramapuram, and Saloni Malla, and Suaad A Audat, and Noor Hussein, and Jenna M Len, and Shikha Kumari, and Mel F Bedi, and Charles R Ashby, and Amit K Tiwari
Design, synthesis, and biological evaluation of novel pyridine-bridged analogues of combretastatin-A4 as anticancer agents.
April 2014, Journal of medicinal chemistry,
Buthina A Al-Oudat, and Hariteja Ramapuram, and Saloni Malla, and Suaad A Audat, and Noor Hussein, and Jenna M Len, and Shikha Kumari, and Mel F Bedi, and Charles R Ashby, and Amit K Tiwari
Design, synthesis and evaluation of novel enzalutamide analogues as potential anticancer agents.
March 2021, Heliyon,
Buthina A Al-Oudat, and Hariteja Ramapuram, and Saloni Malla, and Suaad A Audat, and Noor Hussein, and Jenna M Len, and Shikha Kumari, and Mel F Bedi, and Charles R Ashby, and Amit K Tiwari
Design, synthesis and biological evaluation of 3-substituted-2-oxindole hybrid derivatives as novel anticancer agents.
July 2017, European journal of medicinal chemistry,
Buthina A Al-Oudat, and Hariteja Ramapuram, and Saloni Malla, and Suaad A Audat, and Noor Hussein, and Jenna M Len, and Shikha Kumari, and Mel F Bedi, and Charles R Ashby, and Amit K Tiwari
Synthesis and preliminary biological evaluation of chrysin derivatives as potential anticancer drugs.
January 2010, Medicinal chemistry (Shariqah (United Arab Emirates)),
Copied contents to your clipboard!