A series of novel pyrazolo[3,4-d]pyrimidines was synthesised. Twelve synthesised compounds were evaluated for their anticancer activity against 60 human tumour cell lines by NCI (USA). Compound 7d proved prominent activity. It showed 1.6-fold more potent anti-proliferative OVCAR-4 line with IC50 = 1.74 μM. also exhibited promising ACHN value 5.53 μM, representing 2.2-fold potency than Erlotinib. Regarding NCI-H460 line, compound (IC50 4.44 μM) 1.9-fold inhibited EGFR and ErbB2 kinases at...

New thieno[2,3-d]pyrimidine derivatives were designed and synthesized. The National Cancer Institute (NCI) evaluated the synthesized novel compounds against a panel of 60 tumor cell lines for their antiproliferative activity. Compounds 6b, 6f, 6g showed potent anticancer activity at 10 µM dose, with mean GI 20.86%, 76.41%, 31.49%, respectively. Compound 6f was selected five-dose concentrations evaluation. scored submicromolar range GI50 values cancer lines, indicating broad-spectrum TGI...

New ecofriendly Biginelli reaction procedures have been adapted to prepare new dihydropyrimidines (DHPMs) using a multicomponent one-pot reaction. All the synthesized compounds were evaluated for their anticancer activity against 59 human cancer cell lines and antimicrobial activities representatives of both Gram-positive Gram-negative bacteria. Compound 4 showed marked wide spectrum towards most tested with percentage growth inhibition 29.04–71.68% leukemia line (K-562 SR), lung (NCI-H522),...

Alcoholic fraction of Maclura pomifera fruit extract showed interesting antimicrobial activity when tested in vitro using an agar dilution streak method. [6] Osajin and Pomiferin, two isoflavones previously isolated from this plant, are found to be responsible for the its fruits.

Abstract Fifteen new benzothiophene-based compounds were designed, synthesized, and evaluated as potential anti-Alzheimer agents. Most of the synthesized exhibited remarkable AChE inhibitory activity effectively inhibited self-mediated β-amyloid protein in vitro. Compound 3g (IC 50 = 72.488 ± 3.69 μM) showed a significant effect exceeding that donepezil 87.414 4.46 μM). Furthermore, compound 3j 0.498 0.02 best comparable to 0.404 0.03 The vivo evaluation promising ( ) confirmed memory...

Abstract Novel 3‐phenyltetrahydrobenzo[4,5]thieno[2,3‐ d ]pyrimidine derivatives were synthesized and screened for their antiproliferative activity against a panel of 60 cancer cell lines. Derivatives 5b , 5f 9c showed significant antitumor at single dose with mean growth inhibition 55.62%, 55.79%, 71.40%, respectively. These compounds further investigated HCT‐116, colon line, FHC, normal line. Compound the highest IC 50 = 0.904 ± 0.03 µM SI 20.42 excelling doxorubicin which scored 2.556...

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXT(-)-Misramine: an unusual proaporphine alkaloidSawsan El-Masry, Zeinab Mahmoud, Masouda Amer, Alan J. Freyer, Emir Valencia, Amarendra Patra, and Maurice ShammaCite this: Org. Chem. 1985, 50, 5, 729–730Publication Date (Print):March 1, 1985Publication History Published online1 May 2002Published inissue 1 March 1985https://doi.org/10.1021/jo00205a047Request reuse permissionsArticle Views252Altmetric-Citations15LEARN ABOUT THESE METRICSArticle Views...

Abstract People of all age categories and lifestyles suffer to different extents from hypertension. Accordingly, this necessitates the rise new ways defeat enemy. Vasodilators exert a principal portion highly effectual antihypertensive agents; our research is focused on design, synthesis biological evaluation series 6-(4-substitutedphenyl)-3-pyridazinones as potential hydralazine vasodilator analogues implementing both in vitro silico approaches. All synthesized compounds were assessed for...

Imidazoquinolines are interesting heterocyclic systems that depending on the position of fusion and type substituents display diverse biological pharmaceutical properties.From chemistry point view, imidazoquinolines heterocylic scaffolds resulting from between 5-membered ring imidazole benzopyridine ring, quinoline.At least eight different combinations can be identified for these significant scaffolds.From retrosynthetic prepared using one two general approaches: imidazole-ring formation or...

Alzheimer's Disease (AD) is a multifactorial incurable neurodegenerative disorder. It characterized by decline of cholinergic function in parallel with β-amyloid fibril deposition. Such an imbalance causes severe loss memory and cognition, leading to behavioral disturbances, depression, ultimately death. During the last decades, only few approved drugs were launched onto market indications for treating initial moderate stages AD. To date, cholinesterase inhibitors (ChEI) are mainstay line...

Abstract Alzheimer’s disease (AD) is a multifactorial incurable neurodegenerative disorder. To date, cholinesterase inhibitors (ChEI) are the mainstay line of treatment to ameliorate symptoms AD. Tacrine and donepezil considered two important cornerstones anti-dementia drugs. Accordingly, novel series hexahydrobenzothienocyclopentapyridines, octahydrobenzo-thienoquinolines, hexahydrocyclopenta(thienoquinoline/thienodipyridine), octahydropyrido-thienoquinolines were efficiently synthesized...

Pyrazolo[3,4-d]pyrimidine scaffold was reported to possess potent cytotoxic and CDK2 inhibitory activity as analogue of roscovitine.To design synthesize novel 1-(4-flourophenyl)pyrazolo[3,4-d]pyrimidine derivatives bioisosters roscovitine with potential activity.A series 1-(4-flourophenyl)pyrazolo[3,4-d]pyrimidines were designed synthesized. Structural elucidation for all the newly synthesized compounds achieved through performing MS, 1H NMR, 13C NMR IR spectral techniques. Eight screened...

Repositioning of already approved medications through repurposing or re-profiling for new medical uses after certain structural modifications is a novel approach in drug discovery.

Background.Breast cancer is the most common and leading cause of death for women, a third women are diagnosed with breast at late stage when disease has poor prognosis.Serum tumor markers have been widely used as noninvasive tools measuring treatment response, early diagnosis recurrence predicting prognosis.In cancer, serum antigen 15-3 (CA 15-3) carcinoembryonic (CEA).The aim this study was to investigate association CA15-3 CEA levels clinicopathological parameters in patients metastatic...

Abstract Alzheimer’s disease (AD) is a multifactorial incurable neurodegenerative disorder. To date, cholinesterase inhibitors (ChEI) are the mainstay line of treatment to ameliorate symptoms AD. Tacrine and donepezil considered two important cornerstones as anti-dementia drugs with potent inhibitory effects. Accordingly, novel series hexahydrobenzo-thienocyclopentapyridines, octahydrobenzo-thienoquinolines, hexahydrocyclopenta-(thienoquinoline/thienodipyridine)...