331839-29-3Relevant academic research and scientific papers
High anti-cancer activity, low animal toxicity, and structure activity relationships of curcumin analogs
Song, Sen-Chuan,Mai, Yu-Liang,Shi, Hua-Hong,Liao, Bing,Wang, Fei
, p. 1439 - 1455 (2020/10/06)
Background: Inhibition of cancer cell growth and low in vivo toxicity are two important criteria for the development of anti-cancer drugs. Curcumin is a promising candidate for developing novel anti-cancer drug analogs. The research group designed the 3,5
Synthesis and molecular modeling studies of indole-based antitumor agents
George, Riham F.,Panda, Siva S.,Shalaby, El-Sayed M.,Srour, Aladdin M.,Farag, I. S. Ahmed,Girgis, Adel S.
, p. 45434 - 45451 (2016/06/06)
Indole-based compounds 30-63 were synthesized by the multi-component 1,3-dipolar cycloaddition reaction of 1-alkyl-3,5-bis(arylidene)-4-piperidones 11-25 with azomethine ylides (generated by the condensation of isatins 26-28 with sarcosine 29). The single crystal X-ray studies of 46 and 48 supported the regio- and stereoselectivity of the reaction. Most of the synthesized spiro-indoles exhibited potent antitumor properties against the HeLa (cervical cancer) cell line through in vitro sulfo-rhodamine-B bioassay, higher than that of cisplatin. Only compound 54 showed bio-potency against the HepG2 (hepatocellular cancer) cell line, comparable to that of doxorubicin hydrochloride (standard reference). 3D-Pharmacophore and 2D-QSAR studies were used to validate the observed biological data and determine the most important parameters controlling activity. The estimated bio-properties from the computational studies showed high approximations to the experimental data.
