Synthesis and biological evaluation of novel 3- O -tethered triazoles of diosgenin as potent antiproliferative agents

Masood-ur-Rahman,; Mohammad, Younis; Fazili, Khalid Majid; Bhat, Khursheed Ahmad; Ara, Tabassum

doi:10.1016/j.steroids.2016.11.003

Cited by 58 publications

(23 citation statements)

References 35 publications

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“…In another study Mohammad et al, reported on the anti-proliferative activity of diosgenin and its semi-synthetic derivatives against breast (HBL-100), colon (HCT-116 and HT-19) and lung (A549) cancer cells. A structure-activity relationship study revealed that the potent anti-proliferative activity was mainly attributed to the analogs with the simple phenyl R moiety or electron-withdrawing ortho-substituted R moieties attached to the parent diosgenin [ 86 ]. In another study, diosgenin was used as a parent compound to synthesize 1α-hydroxysolasodine; it showed significant anti-cancer activity against prostate cancer (PC3), cervical carcinoma (HeLa), and hepatocellular carcinoma (HepG2) cells [ 87 ].…”

Section: Semisynthetic Derivatives Of Diosgenin That Exhibit Anti-mentioning

confidence: 99%

Pro-Apoptotic and Anti-Cancer Properties of Diosgenin: A Comprehensive and Critical Review

et al. 2018

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Novel and alternative options are being adopted to combat the initiation and progression of human cancers. One of the approaches is the use of molecules isolated from traditional medicinal herbs, edible dietary plants and seeds that play a pivotal role in the prevention/treatment of cancer, either alone or in combination with existing chemotherapeutic agents. Compounds that modulate these oncogenic processes are potential candidates for cancer therapy and may eventually make it to clinical applications. Diosgenin is a naturally occurring steroidal sapogenin and is one of the major bioactive compounds found in dietary fenugreek (Trigonella foenum-graecum) seeds. In addition to being a lactation aid, diosgenin has been shown to be hypocholesterolemic, gastro- and hepato-protective, anti-oxidant, anti-inflammatory, anti-diabetic, and anti-cancer. Diosgenin has a unique structural similarity to estrogen. Several preclinical studies have reported on the pro-apoptotic and anti-cancer properties of diosgenin against a variety of cancers, both in in vitro and in vivo. Diosgenin has also been reported to reverse multi-drug resistance in cancer cells and sensitize cancer cells to standard chemotherapy. Remarkably, diosgenin has also been reported to be used by pharmaceutical companies to synthesize steroidal drugs. Several novel diosgenin analogs and nano-formulations have been synthesized with improved anti-cancer efficacy and pharmacokinetic profile. In this review we discuss in detail the multifaceted anti-cancer properties of diosgenin that have found application in pharmaceutical, functional food, and cosmetic industries; and the various intracellular molecular targets modulated by diosgenin that abrogate the oncogenic process.

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Section: Semisynthetic Derivatives Of Diosgenin That Exhibit Anti-mentioning

confidence: 99%

Pro-Apoptotic and Anti-Cancer Properties of Diosgenin: A Comprehensive and Critical Review

et al. 2018

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“…It was studied that the compounds with simple phenyl moiety attached through 1,2,3-triazole to the parent molecule 38 demonstrate very high activity against the A549 cancer cell line as compared to the positive control (BEZ-235). 75 The triazolyl pyrimidine hybrids that act as anticancer agents were tested on four cancer cell lines, viz., EC-109 (human esophageal cancer cell line), MCF-7 (human breast cancer cell line), B16-F10 (mouse melanoma cell line), and MGC-803 (human gastric cancer cell line). The results signify the importance of having electron-donating groups on the aryl amine that exhibits high inhibition activity as compared to the compound having electron-withdrawing groups.…”

Section: Introductionmentioning

confidence: 99%

CuAAC-ensembled 1,2,3-triazole-linked isosteres as pharmacophores in drug discovery: review

et al. 2020

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“…17,18 Table 1 showed the list of few phytopharmaceuticals and their therapeutic benefits. [19][20][21][22][23][24][25][26][27][28][29][30][31][32][33][34][35][36][37][38] India has a well-established long history of safe and continuous use of many herbal drugs and phytopharmaceuticals through officially recognized alternative systems of health viz. Ayurveda, Yoga, Unani, Siddha, Homeopathy and Naturopathy.…”

Section: Strengthmentioning

confidence: 99%

Opportunities and Challenges in Development of Phytopharmaceutical Drug in India- A SWOT Analysis

Singh¹,

Kalaivani²,

Srivastava³

et al. 2019

JYP

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Background: India had issued a set of regulation for new class of plant based drug 'Phytopharmaceutical drug' as an amendment to the Drugs and Cosmetic Rules 1945. Age old traditional systems of medicine practiced in India 'Ayurveda', 'Siddha' and 'Unani' medicines. Ayurvedic, Siddha or Unani drugs include all medicines in accordance with the authoritative books of Ayurvedic, Siddha and Unani tibb. systems of medicine specified in the first Schedule of Drugs and Cosmetics Act 1940. Objective: The article aims to analyse opportunities and challenges in development of phytopharmaceutical drug in India through SWOT analysis. Methods: The Strength, Weakness, Opportunities and Threats (SWOT) in development of phytopharmaceutical drug in India was analysed through review of published literatures. Observation: The SWOT analysis showed that India being leader in the herbal industry has massive opportunity in national and international market for phytopharmaceutical drug. It was also observed that the phytopharmaceutical drug market has vital opportunity for expansion both in developed and developing countries. Conclusion: There is a need for investment and commitment in promoting research and development in the area of phytopharmaceutical drug.

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Synthesis and biological evaluation of novel 3- O -tethered triazoles of diosgenin as potent antiproliferative agents

Cited by 58 publications

References 35 publications

Pro-Apoptotic and Anti-Cancer Properties of Diosgenin: A Comprehensive and Critical Review

Pro-Apoptotic and Anti-Cancer Properties of Diosgenin: A Comprehensive and Critical Review

CuAAC-ensembled 1,2,3-triazole-linked isosteres as pharmacophores in drug discovery: review

Opportunities and Challenges in Development of Phytopharmaceutical Drug in India- A SWOT Analysis

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