Rafia Bashir
Hamdard University
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Publication
Featured researches published by Rafia Bashir.
Bioorganic & Medicinal Chemistry Letters | 2011
Rafia Bashir; Syed Ovais; Shafiya Yaseen; Hinna Hamid; Mohammad Sarwar Alam; Mohammad Samim; Surender Singh; Kalim Javed
Thirteen new 2-pyrazoline derivatives bearing benzenesulfonamide moiety (2a-m) were synthesized by condensing appropriate chalcones with 4-hydrazinonbenzenesulfonamide hydrochloride and tested for anticancer and anti-inflammatory actions. According to the protocol of the National Cancer Institute (NCI) in vitro disease-oriented human cells screening panel assay compounds 2b, 2c, 2e, 2f and 2g exhibited considerable antitumor activities against the entire tested tumor cell lines and showed effective growth inhibition GI(50) (MG-MID) values of 2.63, 2.57, 6.61, 3.31 and 2.57μM, respectively, beside a cyclostatic activity TGI (MG-MID) 9.54, 8.51, 24.0, 19.9 and 8.71μM, respectively. Two compounds 2g and 2k showed more potent anti-inflammatory activity than celecoxib at 5h in carrageenan-induced rat paw edema bioassay. These compounds (2g and 2k) proved to have superior gastrointestinal safety profiles as compared to celecoxib, when tested for their ulcerogenic effects. Compounds 2g and 2k showed no inhibition against the enzymatic activity of bovine COX-2 (in vitro).
Bioorganic & Medicinal Chemistry Letters | 2014
Pooja Rathore; Shafiya Yaseen; Syed Ovais; Rafia Bashir; Raed Yaseen; Alhamzah Dh. Hameed; Mohammed Samim; Rakesh Gupta; Firasat Hussain; Kalim Javed
Twenty six new pyrazoline substituted benzenesulfonylureas (2a-z) were synthesized and tested for in vitro anticancer activity. Fourteen derivatives (2i, 2k-2p, 2r, 2s-2x) were screened for their antiproliferative activity towards 60 human cancer cell lines by the National Cancer Institute (USA). Among them four compounds (2i, 2n, 2v and 2x) exhibited significant growth inhibition and further screened at 10-fold dilutions of five different concentrations (0.01, 0.1, 1, 10 and 100 μM). The compounds 2i, 2n, 2v and 2x showed effective growth inhibition (GI50 MID) values of 2.62, 3.93, 3.33, 3.74 μM respectively beside cytostatic activity TGI (MG-MID) values of 8.42, 65.80, 24.00 and 36.06 μM respectively. The compound 2i displayed remarkable antiproliferative activity in 8 different cell lines with GI50 less than 2 μM. Compounds 2n, 2v and 2x also displayed good antiproliferative activity against 11, 18 and 14 different cell lines respectively with GI50 less than 3 μM.
Journal of Enzyme Inhibition and Medicinal Chemistry | 2012
Rafia Bashir; Shafiya Yaseen; Syed Ovais; Shamim Ahmad; Hinna Hamid; M. S. Alam; Mohammad Samim; Kalim Javed
Seven novel 6-aryl-2-(p-sulfamoylphenyl)-4,5-dihydropyridazin-3(2H)-ones (2a-g) were synthesized by the condensation of appropriate aroylpropionic acid and 4-hydrazinobenzenesulfonamide hydrochloride in ethanol. Structure of all compounds have been elucidated by elemental analysis, IR, 1H NMR, 13C NMR, DEPT and MS spectrscopy. These compounds were tested for their anti-inflammatory activity in carrageenan-induced rat paw edema model. Compound 2b exhibited anti-inflammatory activity comparable to that of celecoxib (at 5 h). Two other compounds 2d and 2g showed promising anti-inflammatory activity (edema reduction more than 80% at 5 h). These compounds (2b, 2d and 2g) did not produce any ulceration in gastric region.
European Journal of Medicinal Chemistry | 2014
Syed Ovais; H. Pushpalatha; G. Bhanuprakash Reddy; Pooja Rathore; Rafia Bashir; Shafiya Yaseen; Alhamza Dheyaa; Raed Yaseen; Omprakash Tanwar; Mymoona Akthar; Mohammed Samim; Kalim Javed
Seventeen new pyrazoline substituted benzenesulfonylurea/thiourea derivatives (2a-q) were synthesized and characterized by elemental analysis and various spectroscopic techniques viz; IR, (1)H NMR, (13)C NMR, and MS data. Thirteen compounds showed moderate to good anti-hyperglycaemic activity in glucose fed hyperglycaemic normal rats at the dose of 0.05 mM/kg b.w. On the basis of docking results nine compounds (2a, 2c, 2e, 2h, 2k, 2l, 2n, 2o and 2q) were evaluated for their ability to inhibit rat lens aldose reductase. Out of these six compounds (2h, 2k, 2l, 2n, 2o and 2q) were found more effective than the known ARI sorbinil. Five compounds (2h, 2k, 2l, 2n and 2o) showed significant dual action (anti-hyperglycaemic and aldose reductase inhibition).
Journal of Enzyme Inhibition and Medicinal Chemistry | 2013
Syed Ovais; Shafiya Yaseen; Rafia Bashir; Pooja Rathore; Mohammed Samim; Surender Singh; Vinod Nair; Kalim Javed
Nine novel 4-[3-(4-Dimethylamino-phenyl)-5-aryl-4,5-dihydro-pyrazol-1-yl]-benzenesulfonamides (2a-i) were synthesized and evaluated for their anti-inflammatory and antiproliferative activities. These compounds (2a-i) showed moderate to strong anti-inflammatory activity in carrageenan rat paw oedema test. Compounds 2b, 2d and 2g showing comparable anti-inflammatory activity to that of reference drug celecoxib were evaluated for their ulcerogenic and analgesic activities. The effect of 2b, 2d and 2g on the content of NO, TNF-α and PGE2 in exudates from rat paw stimulated by carrageenan was also evaluated. The compound 2c showed considerable antitumor activities against all 60 human tumor cell lines with effective GI50 (MG-MID) value of 3.63 µM. It exhibited maximum activity against melanoma (LOX IMVI and SK-MEL-5) cancer cell lines with GI50 value less than 2 μM.
Archiv Der Pharmazie | 2013
Shafiya Yaseen; Syed Ovais; Rafia Bashir; Pooja Rathore; Mohammed Samim; Surender Singh; Vinod Nair; Kalim Javed
Nine 4‐arylphthalazones bearing benzenesulfonamide (2a–i) were synthesized by the condensation of the appropriate 2‐aroylbenzoic acid (1a–i) and 4‐hydrazinobenzenesulfonamide in ethanol. The structures of these compounds were elucidated by elemental analysis, IR, 1H NMR, 13C NMR, and MS spectroscopy. Two compounds, 2b and 2i, showed significant anti‐inflammatory activity comparable to that of the standard drug celecoxib in the carrageenan‐induced rat paw edema model. These compounds (2b and 2i) had selective inhibitory activity towards the COX‐2 enzyme. Compound 2b had a better selectivity ratio (COX‐1/COX‐2) compared to that of celecoxib and can be used as a novel template for the design of selective COX‐2 inhibitors. Compounds 2d and 2i were screened for their antiproliferative activity toward 60 human cancer cell lines by the National Cancer Institute (USA). The compounds 2d and 2i displayed mild activity toward the renal cancer cell line UO‐31.
Journal of Enzyme Inhibition and Medicinal Chemistry | 2014
Shafiya Yaseen; Rafia Bashir; Syed Ovais; Pooja Rathore; Mohammed Samim; Kalim Javed
Abstract Some new benzenesulfonylthiourea derivatives substituted with phthalazones (2a–q) were synthesized by refluxing the appropriate 4-aryl-1-oxophthalazin-2(1H)yl benzenesulfonamides with isothiocyanate in dry acetone over anhydrous K2CO3. All the synthesized compounds were characterized on the basis of IR, 1H NMR, MS data and elemental analysis. These synthesized compounds (2a–q) at the dose of 20 mg/kg were tested for antihyperglycemic activity in the glucose-fed hyperglycemic normal rat model and among these compounds 2f and 2m showed modest antihyperglycemic activity.
European Journal of Medicinal Chemistry | 2013
Syed Ovais; Kalim Javed; Shafiya Yaseen; Rafia Bashir; Pooja Rathore; Raed Yaseen; Alhamzah Dh. Hameed; Mohammad Samim
Medicinal Chemistry Research | 2013
Syed Ovais; Rafia Bashir; Shafiya Yaseen; Pooja Rathore; Mohammed Samim; Kalim Javed
Medicinal Chemistry Research | 2012
Rafia Bashir; Shafiya Yaseen; Syed Ovais; Hinna Hamid; M. S. Alam; Mohammad Samim; Kalim Javed