90564-48-0Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of (E)-styrylbenzylsulfones as novel anticancer agents
Reddy, M. V. Ramana,Mallireddigari, Muralidhar R.,Cosenza, Stephen C.,Pallela, Venkat R.,Iqbal, Nabisa M.,Robell, Kimberly A.,Kang, Anthony D.,Reddy, E. Premkumar
, p. 86 - 100 (2008/09/20)
Cell cycle progression is regulated by cyclins and cyclin-dependent kinases, which are formed at specific stages of the cell cycle and regulate the G1/S and G2/M phase transitions, employing a series of "checkpoints" governed by phosphorylation of their substrates. Tumor development is associated with the loss of these checkpoint controls, and this provides an approach for the development of therapeutic agents that can specifically target tumor cells. Here, we describe the synthesis and SAR of a novel group of cytotoxic molecules that selectively induce growth arrest of normal cells in the G1 phase while inducing a mitotic arrest of tumor cells resulting in selective killing of tumor cell populations with little or no effect on normal cell viability. The broad spectrum of antitumor activity in vitro and xenograft models, lack of in vivo toxicity, and drug resistance suggest potential for use of these agents in cancer therapy.
Synthesis and biological evaluation of [4-(2-phenylethenesulfonylmethyl) phenyl]-quinazolin-4-yl-amines as orally active anti-cancer agents
Sharma, Vedula M.,Seshu, K. V. Adi,Sekhar, V. Chandra,Madan, Sachin,Vishnu,Babu, P. Aravind,Krishna, C. Vamsee,Sreenu,Krishna, V. Ravi,Venkateswarlu,Rajagopal, Sriram,Ajaykumar,Kumar, T. Sravan
, p. 67 - 71 (2007/10/03)
A new series of [4-(2-phenylethenesulfonylmethyl)phenyl]quinazolin-4-yl- amines was prepared and tested for its in vitro cytotoxic activity against a panel of 12 human cancer cell lines. Compounds 9, 15, 24 and 31 showed good in vitro activity and were further tested for their in vivo efficacy in the HT-29 human colon adeno carcinoma xenograft model. Compound 9 exhibited promising activity in this model. Dose-response studies for this compound against HT-29 human colon adeno carcinoma xenografts at 100, 200 and 400 mg/kg doses were performed.
