1370351-83-9Relevant academic research and scientific papers
Synthesis of pyrazole-substituted chromene analogues with selective anti-leukemic activity
Madhu,Sudhakar,Santosh Kumar,Rajashekher Reddy,Sravani,Ramakrishna,Prasad Rao, Ch.
, p. 2421 - 2428 (2017/11/24)
We report design and synthesis of a series of flavanone/chromene derivatives containing pyrazoles 6a–6h and 8a–8e with potent anti-leukemic activity. Anti-leukemic activity of novel flavanone derivatives was tested using the K562 cell line. The parental flavanone was selected as the reference compound in identification of analogues with superior anti-leukemic activity. More than two-thirds of the derivatives displayed higher activity than the initial flavanone. Positions of substituents that promoted anti-leukemic activity were identified on both the chromene and pyrazole fragments. Compounds 6b and 6c showed the highest activity against K562 cell line, with IC50 values 3.0 and 0.5 μM respectively. Notably, compounds 6b and 6c displayed very high selectivity in inhibition of leukemic cells (K562) but not of healthy HEK293 cells or solid cancer cell lines HeLa, MCF7 and BT474. Moreover, both the 6b and 6c compounds were predicted to have good ADME properties.
Synthesis and antitumour activity of a novel class of flavanones: 1,4-diaryl-1,4-dihydrochromeno[4,3-c]pyrazoles
Chen, Zhiwei,Wang, Zhihua,Su, Weike
, p. 45 - 48 (2012/04/04)
A new series of 1,4-diaryl-1,4-dihydrochromeno[4,3-c]pyrazoles have been synthesised. The target compounds and their analogues (2,4-diaryl-2,4- dihydrochromeno[4,3-c]pyrazoles) were tested for their antitumour activities in vitro against MCF-7 and HL-60 c
