| Autor: |
Manojkumar R, Shukla, Sukanya, Patra, Mahip, Verma, Gayathri, Sadasivam, Nirmal, Jana, Sachin J, Mahangare, Prashant, Vidhate, Dipak, Lagad, Anand, Tarage, Murthy, Cheemala, Chaitanya, Kulkarni, Shankar, Bhagwat, Vinod D, Chaudhari, Majid, Sayyed, Vipul, Pachpute, Ramesh, Phadtare, Gopal, Gole, Samiron, Phukan, Brahmam, Sunkara, Charudatt, Samant, Manisha, Shingare, Aditya, Naik, Sneha, Trivedi, Ajit Kumar, Marisetti, Madhusudhan, Reddy, Milind, Gholve, Nilesh, Mahajan, Sudeep, Sabde, Vinod, Patil, Dipak, Modi, Maneesh, Mehta, Prashant, Nigade, Kaustubh, Tamane, Swati, Tota, Hemant, Goyal, Harish, Volam, Shashikant, Pawar, Prajakta, Ahirrao, Lal, Dinchhana, Sadanand, Mallurwar, Atul, Akarte, Anand, Bokare, Rupesh, Kanhere, Neetinkumar, Reddy, Sarita, Koul, Manoj, Dandekar, Minakshi, Singh, Peter R, Bernstein, Lakshmi, Narasimham, Mandar, Bhonde, Jayasagar, Gundu, Rajan, Goel, Sanjeev, Kulkarni, Sharad, Sharma, Rajender Kumar, Kamboj, Venkata P, Palle |
| Rok vydání: |
2020 |
| Předmět: |
|
| Zdroj: |
Journal of medicinal chemistry. 63(23) |
| ISSN: |
1520-4804 |
| Popis: |
PI3Kδ inhibitors have been approved for B-cell malignancies like CLL, small lymphocytic lymphoma, and so forth. However, currently available PI3Kδ inhibitors are nonoptimal, showing weakness against at least one of the several important properties: potency, isoform selectivity, and/or pharmacokinetic profile. To come up with a PI3Kδ inhibitor that overcomes all these deficiencies, a pharmacophoric expansion strategy was employed. Herein, we describe a systematic transformation of a "three-blade propeller" shaped lead, 2,3-disubstituted quinolizinone |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
|
