670221-37-1Relevant academic research and scientific papers
Synthesis and evaluation of novel benzophenone-thiazole derivatives as potent VEGF-A inhibitors
Prashanth,Thirusangu, Prabhu,Vijay Avin,Lakshmi Ranganatha,Prabhakar,Khanum, Shaukath Ara
, p. 274 - 283 (2014)
A series of 2-(4-benzoyl-phenoxy)-N-(4-phenyl-thiazol-2-yl)-Acetamides (10a-n) were synthesized by multistep reaction sequence and all the compounds were well characterized for structural elucidation. The in vitro cytotoxicity of compounds 10a-n was evaluated against EAC and DLA cell lines using trypan blue dye exclusion method. Further MTT assay and LDH release assay, followed by in vivo studies on murine model were also evaluated. The compound 10h with a methyl and fluoro groups at benzophenone moiety and methoxy group at phenyl ring was in a leading position to exhibit the promising antiproliferative effect through translational VEGF-A inhibition.
Synthesis, molecular docking, and apoptogenic efficacy of novel N-heterocycle analogs to target B-cell lymphoma 2/X-linked inhibitors of apoptosis proteins to regress melanoma
Zabiulla, Zabiulla,Malojirao, Vikas H.,Mohammed, Yasser Hussein Eissa,Thirusangu, Prabhu,Prabhakar,Khanum, Shaukath Ara
, p. 1132 - 1160 (2019/06/17)
The novel series of piperidine conjugated benzophenone analogs with amide link 11a–l were synthesized in a multistep process. The structures of these compounds were confirmed by IR, 1H, 13C, NMR, and mass spectra and also by elementa
Design and synthesis of diamide-coupled benzophenones as potential anticancer agents
Zabiulla,Shamanth Neralagundi,Bushra Begum,Prabhakar,Khanum, Shaukath Ara
, p. 342 - 351 (2016/04/19)
A series of diamide-coupled benzophenone, 2-(4-benzoyl-phenoxy)-N-{2-[2-(4-benzoyl-phenoxy)-acetylamino]-phenyl}-acetamide analogues (9a-l) were synthesized by multistep reactions and all compounds were well characterized. Among the series (9a-l), compound 9k with three methyl groups at ortho position in rings A, B, and D and bromo group at the para position in ring E was selected as a lead compound by screening through multiple cancer cell types by in-vitro cytotoxic and antiproliferative assay systems. Also, the cytotoxic nature of the compound 9k resulted the regression of the tumor growth in-vivo, which could be due to decreased vascularisation in the peritoneum lining of the mice which regress the tumor growth. The results were reconfirmed in-vivo chorioallantoic membrane model which indicates a scope of developing 9k into potent anticancer drug in near future.
Synthesis, xanthine oxidase inhibition, and antioxidant screening of benzophenone tagged thiazolidinone analogs
Lakshmi Ranganatha,Begum, A. Bushra,Naveen,Zameer, Farhan,Hegdekatte, Raghavendra,Khanum, Shaukath Ara
, p. 589 - 598 (2014/08/18)
A series of novel 2-(diaryl methanone)-N-(4-oxo-2-phenyl-thiazolidin-3-yl)- acetamides were synthesized by various Schiff bases of (4-benzoyl-phenoxy)-aceto hydrazide with thioglycolic acid. The structures of the newly synthesized compounds were confirmed
Design, synthesis, and anticancer properties of novel benzophenone- conjugated coumarin analogs
Lakshmi Ranganatha,Zameer, Farhan,Meghashri,Rekha,Girish,Gurupadaswamy,Khanum, Shaukath Ara
, p. 901 - 911 (2014/01/06)
In the current scenario, development of anticancer drugs with specific targets is of prime importance in modern chemical biology. Observing the importance of benzophenone and coumarin nucleus, it would be worthwhile to design and synthesize novel benzophenone derivatives (8a-o) bearing the coumarin nucleus. Further, they were screened for prospective anticancer activities in vitro against the Michigan Cancer Foundation-7 (MCF-7) and Ehrlich's ascites tumor (EAT) cell lines and their biomarkers, followed by in silico studies regarding phosphoinositide 3-kinase (PI3K) and caspase by molecular docking. Benzophenones have been reported as potential drugs targeting tumor angiogenesis; thus, the formation of neovessels in an in vivo model system like CAM, which is angiogenesis dependent, was observed in the presence of compounds 8a-o. The above findings would help in understanding their putative potential as therapeutic agents for cancer patients. Coumarin-integrated benzophenone conjugates (8a-o) were designed, synthesized, and screened for prospective anticancer activities in vitro against the MCF-7 and EAT cell lines. Molecular docking studies with regard to phosphoinositide 3-kinase and caspase were performed. In addition, neovessel formation was observed in an in vivo model system.
Synthesis and antibacterial activity of various substituted oxadiazole derivatives
Kaur, Hemlata,Kumar, Sunil,Verma,Garg, Amit,Saxena,Lata, Suman,Kumar, Ashok
experimental part, p. 466 - 473 (2012/02/01)
Some new 2-(2-(4(4-substitutedbenzoyl-2-methylphenoxy)acetyl)-N-(2- substitutedphenyl) hydrazinecarbothioamides (4a-4j) and (4-((5-(2- substitutedphenylamino)-1,3,4-oxadiazol-2-yl)methoxy)-3-substitutedphenyl) (phenyl)methanones (5a-5j) have been synthesi
Synthesis of 5-(4′-aroyl)-aryloxy methyl-4H-(1,2,4)-triazolin-3-thiol and their biological activity
Sudha,Shashikanth,Khanum, Shaukath Ara
, p. 85 - 88 (2007/10/03)
5-(4′-aroyl)-aryloxy methyl-4H-1,2, 4)-triazolin-3-thiols were synthesized by using substituted phenyl benzoates as the starting material. Phenyl benzoates on Fries rearrangement gave p-hydroxy benzophenones which on treatment with ethyl bromoacetate in presence of anhydrous potassium carbonate and dry acetone gave corresponding benzoyl phenyloxy esters in excellent yield. Esters were refluxed with thiosemicarbazide in presence of acetic anhydride gave cyclized title compounds. Supports for the structures of the synthesized compounds have been provided by their elemental analysis and spectral data. The newly synthesized compounds were screened for antibacterial and antifungal activities.
Synthesis and antimicrobial activity of 5-[(4-aroyl) aryloxymethyl]-2-(4-methylphenylamino)-1,3,4-thiadiazoles and 5-[(4-aroyl) aryloxy methyl]-4-(4-methylphenyl)-3-mercapto-4H-1,2,4-triazoles
Sudhab,Shashikanth,Khanum, Shaukath Ara
, p. 2652 - 2656 (2007/10/03)
Aroyl aryloxyacetic thiosemicarbazides 4a-d have been synthesized by the reaction of acid hydrazides 3a-d with p-tolyl isothiocyanate. The aroyl aryloxyacetic thiosemicarbazides 4a-d on intramolecular cyclization using conc.H2SO4 and
