In Vitro and In Vivo Anti-Breast Cancer Activities of Some Newly Synthesized 5-(thiophen-2-yl)thieno-[2,3-d]pyrimidin-4-one Candidates.

In this study, some of new thiophenyl thienopyrimidinone derivatives - were prepared and tested as anti-cancer agents by using thiophenyl thieno[2,3-d]pyrimidinone derivative as a starting material, which was prepared from cyclization of ethyl ester derivative with formamide. Treatment of with ethyl- chloroacetate gave thienopyrimidinone -ethylacetate , which was reacted with hydrazine hydrate or anthranilic acid to afford acetohydrazide and benzo[d][1,]oxazin-4-one respectively. Condensation of with aromatic aldehydes or phenylisothiocyanate yielded Schiff base derivatives , and thiosemicarbazise , which were treated with 2-mercaptoacetic acid or chloroacetic acid to give the corresponding thiazolidinones , and phenylimino-thiazolidinone , respectively.

Potent Anti-Ovarian Cancer with Inhibitor Activities on both Topoisomerase II and BRAF of Synthesized Substituted Estrone Candidates.

A series of 16-(α-alkoxyalkane)-17-hydrazino-estra-1(10),2,4-trien[17,16-c]-3-ol (-) and estra-1(10),2,4-trien-[17,16-c]pyrazoline-3-ol derivatives (-) were synthesized from corresponding arylidines which was prepared from estrone as starting material. Condensation of 1 with aldehydes gave the corresponding arylidine derivatives which were treated with hydrazine derivatives in alcohols to give the corresponding derivatives -, respectively. Additionally, treatment of with methyl- or phenylhydrazine in ethanolic potassium hydroxide afforded the corresponding N-substituted pyrazoline derivatives -, respectively.

Retroperitoneal Extrapleural Approach for Corpectomy of the First Lumbar Vertebra : Technique and Outcome.

Objective: Corpectomy of the first lumbar vertebra (L1) for the management of different L1 pathologies can be performed using either an anterior or posterior approach. The aim of this study was to evaluate the usefulness of a retroperitoneal extrapleural approach through the twelfth rib for performing L1 corpectomy.

Methods: Thirty consecutive patients underwent L1 corpectomy between 2010 and 2016.

Socioeconomic restraints and brain tumor surgery in low-income countries.

Healthcare spending has become a grave concern to national budgets worldwide, and to a greater extent in low-income countries. Brain tumors are a serious disease that affects a significant percentage of the population, and thus proper allocation of healthcare provisions for these patients to achieve acceptable outcomes is a must. The authors reviewed patients undergoing craniotomy for tumor resection at their institution for the preceding 3 months.

Multilevel Percutaneous Vertebroplasty (More than Three Levels) in the Management of Osteoporotic Fractures.

Objective: Percutaneous vertebroplasty (PV) is a minimally invasive procedure designed to treat various spinal pathologies. The maximum number of levels to be injected at one setting is still debatable. This study was done to evaluate the usefulness and safety of multilevel PV (more than three vertebrae) in management of osteoporotic fractures.

Synthesis and antimicrobial activity of some new substituted pyrido[3',2':4,5]thieno[3,2-d]-pyrimidinone derivatives.

A series of new 3-substituted-7-(2-chloro-6-ethoxypyridin-4-yl)-9-(2,4-dichlorophenyl)-2-methylpyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4(3H)-one derivatives were synthesized as antimicrobial agents using 7-(2-chloro-6-ethoxypyridin-4-yl)-9-(2,4-dichlorophenyl)-2-methyl-4H-pyrido[3',2':4,5]thieno[3,2-d]-[1,3]oxazin-4-one as a starting compound. Its condensation with substituted aniline derivatives or phenyl hydrazine gave the corresponding N-substituted derivatives. Treatment of the starting compound with hydrazine hydrate afforded the corresponding N-amino derivative, which was reacted with substituted phenylisocyanate and phenylisothiocyanate derivatives to give the corresponding semicarbazides and thiosemicarbazide derivatives.

Androgen receptor antagonists and anti-prostate cancer activities of some newly synthesized substituted fused pyrazolo-, triazolo- and thiazolo-pyrimidine derivatives.

A series of substituted pyrazole, triazole and thiazole derivatives (2-13) were synthesized from 1-(naphtho[1,2-d]thiazol-2-yl)hydrazine as starting material and evaluated as androgen receptor antagonists and anti-prostate cancer agents. The newly synthesized compounds showed potent androgen receptor antagonists and anti-prostate cancer activities with low toxicity (lethal dose 50 (LD50)) comparable to Bicalutamide as reference drug. The structures of newly synthesized compounds were confirmed by IR, 1H-NMR, 13C-NMR, and MS spectral data and elemental analysis.

Anti-parkinsonism, hypoglycemic and anti-microbial activities of new poly fused ring heterocyclic candidates.

A new series of poly fused pyrazolothienopyrimidine derivatives (2-14) were synthesized and their anti-parkinsonism, hypoglycemic and anti-microbial activities were evaluated. Some of the newly synthesized compounds exhibited better pharmacological and biological activities than the reference controls with low concentrations. The structures of newly synthesized compounds were confirmed by chemical, elemental and spectroscopic evidences.

Synthesis of new macrocyclic polyamides as antimicrobial agent candidates.

A series of macrocyclic imides and Schiff-bases have been prepared via the cyclocondensation of pyridine-2,6-dicarbonyl dichloride (1) with L-ornithine methyl ester to give the corresponding macrocyclic bisester 2. Treatment of 2 with hydrazine hydrate gave macrocyclic bisacid hydrazide 3, which was used as starting material. Condensation of bishydrazide 3 with diacid anhydrides or aromatic aldehydes in refluxing acetic acid or ethanol gave the corresponding macrocyclic bisimides 4, 5a,b and macrocyclic bis- hydrazones 6a-j, respectively.

Pharmacological activities of some new polycyclic triazolopyrazolopyridazine derivatives.

In continuation of our previous work, a novel series of polycyclic derivatives were synthesized and their anti-inflammatory, analgesic and antimicrobial activities were evaluated. Initially the acute toxicity of the compounds was assayed via the determination of their LD(50). Some of the newly compounds exhibited better biological and pharmacological activities than the reference controls with low toxicity (LD(50)).

Androgen receptor antagonists and anti-prostate cancer activities of some synthesized steroidal candidates.

In continuation of our previous work, a novel series of steroid derivatives were synthesized and their androgen receptor (AR) antagonist activities and in vivo antiandrogenic properties were evaluated. Twenty-one heterocyclic derivatives containing a cyanopyrane ring fused to a steroidal moiety were conveniently synthesized and screened for their antagonistic, antiandrogen and prostate anticancer activities comparable to that of bicalutamide as the reference control. Some of the compounds exhibited better antagonistic, antiandrogen and prostate anticancer activities than the reference controls.