314745-06-7Relevant academic research and scientific papers
Novel Chrysin-de-allyl PAC-1 hybrid analogues as anticancer compounds: Design, synthesis, and biological evaluation
Al-Oudat, Buthina A.,Ashby, Charles R.,Audat, Suaad A.,Bedi, Mel F.,Hussein, Noor,Kumari, Shikha,Le, Jenna M.,Malla, Saloni,Ramapuram, Hariteja,Tiwa, Amit K.
, (2020)
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.
Design, synthesis, and biologic evaluation of novel chrysin derivatives as cytotoxic agents and caspase-3/7 activators
Al-Oudat, Buthina Abdallah,Al-Balas, Qosay Ali,El-Elimat, Tamam,Hassan, Mohammad Abdelhafeez,Frhat, Islam Nawaf,Alqudah, Mohammad Ali,Azaizeh, Marwah Mohammad,Audat, Suaad Abdallah
, p. 423 - 433 (2019)
Background: Chrysin (5,7-dihydroxyflavone) is a widely distributed natural flavonoid found in many plant extracts, honey and propolis. Several studies revealed that chrysin possesses multiple biological activities including anti-cancer effects. It has bee
NO donor compounds, compositions, preparation method and application thereof
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Paragraph 0270; 0271-0274, (2019/11/13)
The object of the present invention is to provide NO donor compounds, compositions, a preparation method and application thereof. The compounds and the compositions show high anticancer activity in in-vitro anticancer activity tests, and have inhibitory a
Structure-based design of flavone-based inhibitors of wild-type and T315I mutant of ABL
Choe, Hyeonjeong,Kim, Jieun,Hong, Sungwoo
supporting information, p. 4324 - 4327 (2013/07/25)
The existence of drug resistance caused by mutations in the break-point cluster region-Abelson (BCR-ABL) tyrosine kinase domain remains a clinical challenge due to limited treatment options for effective CML therapies. Here, we report a series of flavone-based common inhibitors equipotent for the wild type and the most drug-resistant T315I mutant of BCR-ABL. The original hit 1 was extensively modified through a structure-based drug design strategy, especially by varying the C7 acetamide appendage of the scaffold to exploit extended interactions with P-loop residues. Structural features relevant to the stabilization of the newly identified inhibitors in the ATP-binding site of ABL are discussed in detail.
