Recent advancement of piperidine moiety in treatment of cancer- A review

Goel, Pallavi; Alam, Ozair; Naim, Mohd. Javed; Nawaz, Farah; Iqbal, Muzaffar; Alam, Iqbal

doi:10.1016/j.ejmech.2018.08.017

Cited by 112 publications

(51 citation statements)

References 144 publications

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“…[11] A large portion of therapeutic agents and biologically active molecules are also known to contain the substituted-piperidine scaffolds. [12,13] Therefore, the development of efficient methods for the construction of chiral piperidine frameworks especially from cheap and readily available precursors has remained an attractive synthetic endeavor due to their highly esteemed prospect for both medicinal and pharmaceutical applications. [14] Herein, we will disclose a highly enantioselective organocatalyst 1-mediated asymmetric Michael reaction of aldehydes 2 and α-cyano α,β-unsaturated esters 3.…”

Section: Asymmetric Michael Reaction Of Aldehydes and α-Cyano αβ-Unsmentioning

confidence: 99%

Asymmetric Michael Reaction of Aldehydes and α‐Cyano α,β‐Unsaturated Esters Catalyzed by Diphenylprolinol Silyl Ether; a Facile Asymmetric Route to 3,4,5‐Trisubstituted Piperidines

2020

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Section: Asymmetric Michael Reaction Of Aldehydes and α-Cyano αβ-Unsmentioning

confidence: 99%

Asymmetric Michael Reaction of Aldehydes and α‐Cyano α,β‐Unsaturated Esters Catalyzed by Diphenylprolinol Silyl Ether; a Facile Asymmetric Route to 3,4,5‐Trisubstituted Piperidines

2020

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“…Piperidine is a privileged scaffold in the field of drug discovery which provides numerous opportunities in exploring this moiety as an anticancer agent by acting on various receptors of utmost importance ( Figure 2) 14 . Pomalidomide (7) was a FDA approved drug to treat multiple myeloma by inhibiting TNF a 15 .…”

Section: Introductionmentioning

confidence: 99%

Novel piperidine derivatives as colchicine binding site inhibitors induce apoptosis and inhibit epithelial-mesenchymal transition against prostate cancer PC3 cells

Liu

Yang

et al. 2020

Journal of Enzyme Inhibition and Medicinal Chemistry

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Tubulin polymerisation inhibitors that target colchicine binding site were powerful anticancer agents. Although along the years many colchicine binding site inhibitors (CBSIs) have been reported, few piperidine derivatives were identified as CBSIs. In this regard, we focussed efforts on the piperidine as a promising chemotype to develop potent CBSIs. Herein, novel piperidine derivatives were synthesised and evaluated for their antiproliferative activities. Among them, compound 17a displayed powerful anticancer activity with the IC 50 value of 0.81 mM against PC3 cells, which was significantly better than 5-fluorouracil. It could inhibit tubulin polymerisation binding at the colchicine site and inhibit the tumour growth in vitro and in vivo. Further biological studies depicted that 17a suppressed the colony formation, induced apoptosis, and inhibited epithelial-mesenchymal transition against PC3 cells. These results revealed that compound 17a is a promising colchicine binding site inhibitor for the treatment of cancer and it is worthy of further exploitation.

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“…It is the second leading cause of death, after cardiovascular disease, worldwide [1,2]. The World Health Organization has reported that there were approximately 17.5 million new cancer cases and more than 8.7 million cancer-related deaths worldwide in 2015, and cancer-related deaths are expected to increase to 13.1 million by 2030 [3,4,5]. Cancer is a type of abnormal and excessive growth of tissue, in which abnormal body cells begin to divide uncontrollably by ignoring the principles of normal cell division.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Cucurbitacin B Derivatives as Potential Anti-Hepatocellular Carcinoma Agents

Chen

Han

et al. 2018

Molecules

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Cucurbitacin B shows potent activity against tumor cells, but its high toxicity limits its application in the clinic. A series of cucurbitacin B derivatives was synthesized and evaluated for their anti-hepatocellular carcinoma (HCC) activities against the HepG-2 cell line. These compounds were also tested for their toxicity against the L-O2 normal cell line. The compound with the most potential, 10b, exhibited potent activity against the HepG-2 cell line with an IC50 value of 0.63 μM. Moreover, compound 10b showed the highest TI value (4.71), which is a 14.7-fold improvement compared to its parent compound cucurbitacin B. A preliminary molecular mechanism study of 10b indicated that 10b could inhibit P-STAT3 to induce the activation of mitochondrial apoptotic pathways. An in vivo acute toxicity study indicated that the compound 10b has preferable safety and tolerability compared with cucurbitacin B. These findings indicate that compound 10b might be considered as a lead compound for exploring effective anti-HCC drugs.

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Recent advancement of piperidine moiety in treatment of cancer- A review

Cited by 112 publications

References 144 publications

Asymmetric Michael Reaction of Aldehydes and α‐Cyano α,β‐Unsaturated Esters Catalyzed by Diphenylprolinol Silyl Ether; a Facile Asymmetric Route to 3,4,5‐Trisubstituted Piperidines

Asymmetric Michael Reaction of Aldehydes and α‐Cyano α,β‐Unsaturated Esters Catalyzed by Diphenylprolinol Silyl Ether; a Facile Asymmetric Route to 3,4,5‐Trisubstituted Piperidines

Novel piperidine derivatives as colchicine binding site inhibitors induce apoptosis and inhibit epithelial-mesenchymal transition against prostate cancer PC3 cells

Synthesis of Cucurbitacin B Derivatives as Potential Anti-Hepatocellular Carcinoma Agents

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