Novel modified steroid derivatives of androstanolone as chemotherapeutic anti-cancer agents

El‐Far, Mohamed; Elmegeed, Gamal A.; Eskander, Emad F.; Rady, Hanaa M.; Tantawy, Mohamed A.

doi:10.1016/j.ejmech.2009.04.020

Cited by 83 publications

(27 citation statements)

References 20 publications

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“…In light of the above discoveries, and in continuation of studies involving the synthesis of novel biologically active modified steroids [9,12,13]. In the present study, some novel steroid hybrids incorporating the pyrrole or thiazole moiety through different linkages have been developed and it is expected to exhibit anti-inflammatory, anti-nociceptive, and/or non-ulcerogenic activities.…”

Section: Introductionmentioning

confidence: 97%

Evaluation of Anti‐inflammatory, Anti‐nociceptive, and Anti‐ulcerogenic Activities of Novel Synthesized Thiazolyl and Pyrrolyl Steroids

Mohareb

Elmegeed

Baiuomy

et al. 2011

Archiv der Pharmazie

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Developing new therapeutic agents that can overcome gastrointestinal injury and at the same time could lead to an enhanced anti-inflammatory effect becomes an urgent need for inflammation patients. Thiazolyl and pyrrolyl steroids were synthesized via straight forward and efficient methods and their structures were established based on their correct elemental analysis and compatible IR, (1) H-NMR, (13) C-NMR, and mass spectral data. The dihydrothiazolyl-hydrazonoprogesterone 12 and the aminopyrrolylprogesterone 16a showed anti-inflammatory, antinociceptive, and anti-ulcerogenic activity with various intensities. Edema were significantly reduced by both doses of tested compounds (25 and 50 mg/kg) at 2, 3, and 4 h post-carrageenan. The high dose of compound 16a was the most effective in alleviating thermal pain. Gastric mucosal lesions, caused in the rats by the administration of ethanol or indomethacin (IND), were significantly inhibited by each of the two tested compounds. These results provide a unique opportunity to develop new anti-inflammatory drugs which devoid the ulcerogenic liabilities associated with currently marketed drugs.

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Section: Introductionmentioning

confidence: 97%

Evaluation of Anti‐inflammatory, Anti‐nociceptive, and Anti‐ulcerogenic Activities of Novel Synthesized Thiazolyl and Pyrrolyl Steroids

Mohareb

Elmegeed

Baiuomy

et al. 2011

Archiv der Pharmazie

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“…This study motivated us to assemble newer and more widely effective kinase inhibitors. Our synthetic approach is based on the concept of molecular hybridization, an effective tool for the cogent design of novel molecular constructs by covalently conjugating two or more active pharmacophores [24]. Such constructs are known to exhibit improved pharmacokinetic-dynamic properties, potency to act on more than one target with reduced side effects and efficacy in case of drug resistant cases [25].…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, and Evaluation of the Kinase Inhibition Potential of Pyridylpyrimidinylaminophenyl Derivatives

Manchanda

Parshad

Kumar

et al. 2017

Archiv der Pharmazie

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In view of potent kinase inhibitors for the treatment of myriad human disorders, we synthesized some structurally variant amide/cyclic amide derivatives based on pyridylpyrimidinylaminophenyl amine, the key pharmacophore of the kinase inhibitor drug molecule, imatinib, and evaluated their kinase inhibition potency. Among the various synthesized amides, compound 20, a cyclic amide/pyridin-2(1H)-one derivative, exhibited an IC value comparable to that of the drug imatinib against c-Src kinase, and another compound (14) containing a 2-((4-methyl-2-oxo-2H-chromen-6-yl)oxy)acetamide demonstrated an IC value of 8.39 μM. Furthermore, the constitution of the cyclic amide derivative was confirmed by the single-crystal X-ray diffraction technique. These results may serve as a gateway for developing novel next-generation kinase inhibitors.

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“…The clubbed pharmacophores may act on multiple therapeutic targets and offer the advantage of overcoming inevitable drug resistance [16]. In addition, the hybrids may also minimize unwanted side effects and allow for synergistic action [17]. The molecular hybrid approach has already been applied in developing novel antimalarial agents to overcome drug resistance [18].…”

Section: Introductionmentioning

confidence: 99%

Design and Synthesis of Novel Triazolyl Benzoxazine Derivatives and Evaluation of Their Antiproliferative and Antibacterial Activity

Khan

Prasad

Parmar

et al. 2015

Journal of Heterocyclic Chem

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A series of novel triazolyl benzoxazine derivatives have been synthesized via Cu(I)‐catalyzed ‘Click’ cycloaddition. All of the compounds were fully characterized from their spectral data, and their antiproliferative activity was evaluated against three selected human cancer cell lines: cervical cancer cells (HeLa), colorectal adenocarcinoma (HT‐29), and ovarian adenocarcinoma (SKOV‐3). A few representative compounds have also been evaluated for their antibacterial potential against two bacterial strains Pseudomonas aeruginosa and Bacillus subtilis.

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Novel modified steroid derivatives of androstanolone as chemotherapeutic anti-cancer agents

Cited by 83 publications

References 20 publications

Evaluation of Anti‐inflammatory, Anti‐nociceptive, and Anti‐ulcerogenic Activities of Novel Synthesized Thiazolyl and Pyrrolyl Steroids

Evaluation of Anti‐inflammatory, Anti‐nociceptive, and Anti‐ulcerogenic Activities of Novel Synthesized Thiazolyl and Pyrrolyl Steroids

Design, Synthesis, and Evaluation of the Kinase Inhibition Potential of Pyridylpyrimidinylaminophenyl Derivatives

Design and Synthesis of Novel Triazolyl Benzoxazine Derivatives and Evaluation of Their Antiproliferative and Antibacterial Activity

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