Promising applications of steroid сonjugates for cancer research and treatment

Zolottsev, Vladimir A.; Latysheva, Alexandra S.; Pokrovsky, Vadim S.; Khan, Irina I.; Misharin, A. Yu.

doi:10.1016/j.ejmech.2020.113089

Cited by 21 publications

(12 citation statements)

References 83 publications

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“…Recently, several reviews highlighting the varied therapeutic significance of steroid–amino acid conjugates and bile acid–bioactive molecule conjugates have been published. The therapeutic use of steroidal bioconjugates in cancer therapy has also been widely explored as indicated by numerous relevant literature reports. − In light of this, we thought it worthwhile to present a comprehensive review on the structurally diverse steroidal bioconjugates of potential therapeutic interest. This review covers the potential biological applications of steroidal bioconjugates and would benefit the wider scientific community in their drug discovery endeavors.…”

Section: Steroidal Bioconjugatesmentioning

confidence: 99%

A Comprehensive Review on Steroidal Bioconjugates as Promising Leads in Drug Discovery

Bansal

Suryan

2022

ACS Bio Med Chem Au

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Ever increasing unmet medical requirements of the human race and the continuous fight for survival against variety of diseases give birth to novel molecules through research. As diseases evolve, different strategies are employed to counter the new challenges and to discover safer, more effective, and target-specific therapeutic agents. Among several novel approaches, bioconjugation, in which two chemical moieties are joined together to achieve noticeable results, has emerged as a simple and convenient technique for a medicinal chemist to obtain potent molecules. The steroid system has been extensively used as a privileged scaffold gifted with significantly diversified medicinal properties in the drug discovery and development process. Steroidal molecules are preferred for their rigidness and good ability to penetrate biological membranes. Slight alteration in the basic ring structure results in the formation of steroidal derivatives with a wide range of therapeutic activities. Steroids are not only active as such, conjugating them with various biologically active moieties results in increased lipophilicity, stability, and target specificity with decreased adverse effects. Thus, the steroid nucleus prominently behaves as a biological carrier for small molecules. The steroid bioconjugates offer several advantages such as synergistic activity with fewer side effects due to reduced dose and selective therapy. The steroidal bioconjugates have been widely explored for their usefulness against various disorders and have shown significant utility as anticancer, anti-inflammatory, anticoagulant, antimicrobial, insecticidal/pesticidal, antioxidant, and antiviral agents along with several other miscellaneous activities. This work provides a comprehensive review on the therapeutic progression of steroidal bioconjugates as medicinally active molecules. The review covers potential biological applications of steroidal bioconjugates and would benefit the wider scientific community in their drug discovery endeavors.

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Section: Steroidal Bioconjugatesmentioning

confidence: 99%

A Comprehensive Review on Steroidal Bioconjugates as Promising Leads in Drug Discovery

Bansal

Suryan

2022

ACS Bio Med Chem Au

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“…[72,73] 7 | 1,2,3-TRIAZOLE-STEROID/TERPENE HYBRIDS Steroids and terpenes, widely distributed in the plant kingdom, not only could act as inhibitors of various enzymes, proteins, and receptors in cancer cells, but also exhibited low cytotoxicity, high bioavailability, and potential against various cancers including multidrug-resistant forms. [74,75] Some steroids and terpenes could exert antileukemic activity through various pathways including the activation of mitochondrial apoptosis, whereas some of them are deemed as sensitizing leukemia cells to the chemotherapeutic effects of many cytotoxic agents, primarily by inhibiting efflux pumps, thus reducing leukemia resistance. [76,77] Accordingly, a combination of 1,2,3-triazole with steroid/terpene is a promising strategy to develop novel antileukemic chemotherapeutics.…”

Section: 23-triazole-naphthoquinone Hybridsmentioning

confidence: 99%

Therapeutic potential of 1,2,3‐triazole hybrids for leukemia treatment

Yang¹,

Xuan²,

Li³

et al. 2022

Archiv der Pharmazie

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Leukemia, a hematological malignancy originating from the bone marrow, is the principal cancer of childhood. In recent decades, improved remission rates and survival of patients with leukemia have been achieved due to significant breakthroughs in the treatment. However, chemoresistance and relapse are common, creating an urgent need for the search for novel pharmaceutical interventions. 1,2,3‐Triazole is one of the most fascinating pharmacophores in the discovery of new drugs, and several 1,2,3‐triazole derivatives have already been used in clinics or are under clinical evaluation for the treatment of cancers. In particular, 1,2,3‐triazole hybrids could suppress tumor proliferation, invasion, and metastasis by inhibiting enzymes, proteins, and receptors in cancer cells, revealing their potential as putative antileukemic agents. This review covers the recent advances regarding the 1,2,3‐triazole hybrids with potential antileukemic activity, focusing on the chemical structures, structure–activity relationship, and mechanisms of action, covering articles published from January 2017 to January 2022.

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“…As of September 2019, approximately 84.3% (156 out of 185) of anticancer small molecules approved by the FDA are natural products or their derivatives 1 , which affirms the position of natural products as a focal point for finding structural and medicinal inspiration for drug discovery. Natural steroids and their synthetic derivatives are attracting increasing research interest for their promising anti-tumour activities and potential utilisation in the discovery and design of new anti-tumour agents 2–4 .…”

Section: Introductionmentioning

confidence: 99%

Design, synthesis and biological evaluation of novel diosgenin–benzoic acid mustard hybrids with potential anti-proliferative activities in human hepatoma HepG2 cells

Zhang

Wang

Tian

et al. 2022

Journal of Enzyme Inhibition and Medicinal Chemistry

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To discover new lead compounds with anti-tumour activities, in the present study, natural diosgenin was hybridised with the reported benzoic acid mustard pharmacophore. The in vitro cytotoxicity of the resulting newly synthesised hybrids ( 8 – 10 , 14a – 14f , and 15a – 15f ) was then evaluated in three tumour cells (HepG2, MCF-7, and HeLa) as well as normal GES-1 cells. Among them, 14f possessed the most potential anti-proliferative activity against HepG2 cells, with an IC 50 value of 2.26 µM, which was 14.4-fold higher than that of diosgenin (IC 50 = 32.63 µM). Furthermore, it showed weak cytotoxicity against GES-1 cells (IC 50 > 100 µM), thus exhibiting good antiproliferative selectivity between normal and tumour cells. Moreover, 14f could induce G0/G1 arrest and apoptosis of HepG2 cells. From a mechanistic perspective, 14f regulated cell cycle-related proteins (CDK2, CDK4, CDK6, cyclin D1 and cyclin E1) as well mitochondrial apoptosis pathway-related proteins (Bax, Bcl-2, caspase 9, and caspase 3). These findings suggested that hybrid 14f serves as a promising anti-hepatoma lead compound that deserves further research.

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Promising applications of steroid сonjugates for cancer research and treatment

Cited by 21 publications

References 83 publications

A Comprehensive Review on Steroidal Bioconjugates as Promising Leads in Drug Discovery

A Comprehensive Review on Steroidal Bioconjugates as Promising Leads in Drug Discovery

Therapeutic potential of 1,2,3‐triazole hybrids for leukemia treatment

Design, synthesis and biological evaluation of novel diosgenin–benzoic acid mustard hybrids with potential anti-proliferative activities in human hepatoma HepG2 cells

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