Synthesis, cytotoxic characterization, and SAR study of imidazo[1,2-b]pyrazole-7-carboxamides
The synthesis and in vitro cytotoxic characteristics of new imidazo[1,2-b]pyrazole-7-carboxamides were investigated. Following a hit-to-lead optimization exploiting 2D and 3D cultures of MCF-7 human breast, 4T1 mammary gland, and HL-60 human promyelocytic leukemia cancer cell lines, a 67-membered li...
Elmentve itt :
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| Dokumentumtípus: | Cikk |
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2018
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| Sorozat: | ARCHIV DER PHARMAZIE
351 No. 7 |
| doi: | 10.1002/ardp.201800062 |
| mtmt: | 3399467 |
| Online Access: | http://publicatio.bibl.u-szeged.hu/14531 |
| Tartalmi kivonat: | The synthesis and in vitro cytotoxic characteristics of new imidazo[1,2-b]pyrazole-7-carboxamides were investigated. Following a hit-to-lead optimization exploiting 2D and 3D cultures of MCF-7 human breast, 4T1 mammary gland, and HL-60 human promyelocytic leukemia cancer cell lines, a 67-membered library was constructed and the structure-activity relationship (SAR) was determined. Seven synthesized analogues exhibited sub-micromolar activities, from which compound 63 exerted the most significant potency with a remarkable HL-60 sensitivity (IC50=0.183M). |
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| Terjedelem/Fizikai jellemzők: | Paper e1800062-21 p. |
| ISSN: | 0365-6233 |