Design and Synthesis of 3, 5-Diphenylpyrazole derivatives as Selective Estrogen Receptor Modulators

نویسندگان

چکیده

This exploratory work encompasses synthetic chemistry to develop novel 3, 5- diphenylethanone derivatives compounds based on the medicinally relevant scaffold of pyrazole as that standard SERM i.e. Tamoxifen and Raloxifene. Specific strategies for synthesis analogues were used subjected modeling docking studies analyzing ER subtype selectivity. The in-silico conducted in order attain a better insight into interactions these molecules with their target receptor study selectivity preferential binding site. various orientations taken by ligands while estrogen receptor-α studied over 1ERR (PDB) using Schrodinger Maestro environments. anti-cancer potential evaluated receptor-positive cell lines an vitro assay, exploring MCF-7 Zr-75-1 lines. Amongst all, displaced promising anticancer activity (4-chloro substituted, compound 4b) selectively screened vivo NMU administration mammary carcinoma female Sprague- Dawley rat. As hormone has been largely implemented metastasis breast cancer, it become imperative measure levels tumor-affected animals. percentage incidences, tumor latency, burden, volume was measured after sacrificing experimental

برای دانلود باید عضویت طلایی داشته باشید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Genistein derivatives as selective estrogen receptor modulators: sonochemical synthesis and in vivo anti-osteoporotic action.

Genistein derivatives were synthesized from genistein through a facile sonochemical approach in high yields. The bioassay was performed on ovariectomized (OVX) rats in terms of bone mineral density (BMD) and the weight of bone ash (WBA) to lead to the discovery of eight novel genistein-based selective estrogen receptor modulators. Attention to the structure-activity relationship disclosed that ...

متن کامل

Design, Synthesis and Biological Evaluation of 5-Oxo-1,4,5,6,7,8 Hexahydroquinoline Derivatives as Selective Cyclooxygenase-2 Inhibitors

A group of regioisomeric 5-oxo-1,4,5,6,7,8 hexahydroquinoline derivatives possessing a COX-2 SO2Me pharmacophore at the para position of the C-2 or C-4 phenyl ring, in conjunction with a C-4 or C-2 phenyl (4-H) or substituted-phenyl ring (4-F,4-Cl,4-Br,4-OMe,4-Me, 4-NO2), were designed for evaluation as selective cyclooxygenase-2 (COX-2) inhibitors. These target 5-oxo-1,4,5,6,7,8 hexahydroquino...

متن کامل

Design, Synthesis and Biological Evaluation of 5-Oxo-1,4,5,6,7,8 Hexahydroquinoline Derivatives as Selective Cyclooxygenase-2 Inhibitors

A group of regioisomeric 5-oxo-1,4,5,6,7,8 hexahydroquinoline derivatives possessing a COX-2 SO2Me pharmacophore at the para position of the C-2 or C-4 phenyl ring, in conjunction with a C-4 or C-2 phenyl (4-H) or substituted-phenyl ring (4-F,4-Cl,4-Br,4-OMe,4-Me, 4-NO2), were designed for evaluation as selective cyclooxygenase-2 (COX-2) inhibitors. These target 5-oxo-1,4,5,6,7,8 hexahydroquino...

متن کامل

Selective Estrogen Receptor Modulators

Selective estrogen receptor modulators (SERMs) are now being used as a treatment for breast cancer, osteoporosis and postmenopausal symptoms, as these drugs have features that can act as an estrogen agonist and an antagonist, depending on the target tissue. After tamoxifen, raloxifene, lasofoxifene and bazedoxifene SERMs have been developed and used for treatment. The clinically decisive differ...

متن کامل

Selective estrogen receptor modulators (SERMS).

Hormone receptors and, specifically, estrogen receptors were described about four decades ago. For estrogens, there are two receptors, estrogen receptor alpha (ERalpha) and estrogen receptor beta (ERbeta). The two receptors are coded by different genes and their tissue expression varies across organs. ERalpha is predominantly expressed in reproductive tissues (uterus, breast, ovaries) liver and...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

ژورنال

عنوان ژورنال: International Journal of Research in Pharmaceutical Sciences

سال: 2022

ISSN: ['0975-7538']

DOI: https://doi.org/10.26452/ijrps.v13i3.1778