Journal ArticleDOI
Synthesis and antileukemic activity of novel 4‐(3‐(piperidin‐4‐yl) propyl) piperidine derivatives
K. Vinaya,K. Vinaya,C. V. Kavitha,C. V. Kavitha,S. Chandrappa,D. S. Prasanna,Sathees C. Raghavan,Kanchugarakoppal S. Rangappa +7 more
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TLDR
The most active compound among this series was 3a with nitro and fluoro substitution on the phenyl ring of aryl carboxamide moiety, which inhibited the growth of human leukemia cells at low concentration.Abstract:
To explore the anticancer effect associated with the piperidine framework, several (substituted phenyl) {4-[3-(piperidin-4-yl)propyl]piperidin-1-yl} methanone derivatives 3(a-i) were synthesized. Variation in the functional group at N-terminal of the piperidine led to a set of compounds bearing amide moiety. Their chemical structures were confirmed by (1) H NMR, IR and mass spectra analysis. Among these, compounds 3a, 3d and 3e were endowed with antiproliferative activity. The most active compound among this series was 3a with nitro and fluoro substitution on the phenyl ring of aryl carboxamide moiety, which inhibited the growth of human leukemia cells (K562 and Reh) at low concentration. Comparison with other derivative (3h) results shown by LDH assay, cell cycle analysis and DNA fragmentation suggested that 3a is more potent to induce apoptosis.read more
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Recent advancement of piperidine moiety in treatment of cancer- A review.
TL;DR: This review throws light on recent biological expansions of piperidine along with structure activity relationships to deliver association between various synthesized newer/novel derivatives and receptor sites.
Journal ArticleDOI
Synthesis and antiproliferative effect of novel 4-thiazolidinone-, pyridine- and piperazine-based conjugates on human leukemic cells.
Kothanahally S. Sharath Kumar,Ananda Hanumappa,Mahesh Hegde,Kereyagalahally H. Narasimhamurthy,Sathees C. Raghavan,Kanchugarakoppal S. Rangappa +5 more
TL;DR: Cell cycle analysis and mitochondrial membrane potential further confirmed that compound 5 is cytotoxic and able to induce cell death.
Journal ArticleDOI
Synthesis, Crystal Structure, and Fungicidal Activity of a Novel 1,2,3-Thiadiazole Compound
TL;DR: A new 1,2,3-thiadiazole compound, C18H18Cl2N4O2S, has been synthesized and the crystal structure was determined by single crystal X-ray diffraction study.
Journal ArticleDOI
Synthesis and antiproliferative studies of curcumin pyrazole derivatives
Honnalagere Ramesh Puneeth,Hanumappa Ananda,Kothanahally S. Sharath Kumar,Kanchugarakoppal S. Rangappa,A. C. Sharada +4 more
TL;DR: The findings suggest that compound 3b could be a promising anticancer agent since it effectively inhibited cell proliferation and can be selected for further in vitro and in vivo investigations.
Journal ArticleDOI
Design, synthesis and biological evaluation of novel arylpiperazine derivatives on human prostate cancer cell lines.
TL;DR: A series of novel arylpiperazine derivatives was synthesized and in vitro cytotoxic activities of all synthesized compounds against three human prostate cancer cell lines were evaluated by a CCK-8 assay.
References
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Novel derivatives of spirohydantoin induce growth inhibition followed by apoptosis in leukemia cells
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Journal ArticleDOI
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Journal ArticleDOI
Synthesis of 2-(5-((5-(4-chlorophenyl)furan-2-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)acetic acid derivatives and evaluation of their cytotoxicity and induction of apoptosis in human leukemia cells.
S. Chandrappa,C. V. Kavitha,M. S. Shahabuddin,K. Vinaya,C. S. Ananda Kumar,S. R. Ranganatha,Sathees C. Raghavan,Kanchugarakoppal S. Rangappa +7 more
TL;DR: It was concluded that the 4th position of the substituted aryl ring plays a dominant role for its anticancer property and two molecules (5e and 5k) having different electron donating group at different positions are rationalized in the induction of cytotoxicity.