The chemistry and an extensive spectrum of biological activities of spirooxindole have been examined since several decades and this heterocyclic core has received emerging consensus. This content aims to summarize recent advances made towards the discovery of Antituberculosis activity, AChE and BChE inhibitory activity, Anti-tumor activity, Antibacterial and Antifungal activity and Miscellaneous Activity holding spirooxindole as a nucleus with the substitution of several types of nucleophiles, and molecular patterns associated with particular potency have been identified targeting several Gram-positive and Gram-negative bacteria and some fungal species, mycobacterium tuberculosis H37Rv, and drug-resistant tuberculosis (XDR-TB), Alzheimer's disease, HCT 116 (colon), MCF 7 (Brest) and HEPG 2 (liver) human tumor cell lines. The report will be of enormous interest to gain useful information for the furtherance of drug discovery with extended spirooxindole designs.
Cancer is one of the most dreaded diseases responsible for millions of deaths every year. In the present study, 12 medicinal plants from Jammu region, viz., Alstonia scholaris (devil tree), Azadirachta indica (neem), Calotropis gigantea (milk weed), Emblica officinalis (amla), Mentha citrata (bergamot mint), Mentha piperita (piper mint), Mentha viridis (pudina), Murraya koengii (kari pata), Musa paradisiaca (banana), Olea europaea (olive), Punica garanatum (pomegranate) and Trachyspermum ammi (ajwain) were evaluated against five human cancer cell lines from four different origins, viz., A-549 (lung), HCT-116 (colon), MCF-7 (breast), PC-3 (prostate) and T-47D (breast). 7 medicinal plants showed in vitro cytotoxic effect against one or the other human cancer cell line with the remarkable results produced by Calotropis gigantea (73-78% growth inhibition at 10 mig/ml against lung, colon and prostate cancer cells).To conclude, the plant can provide a great service and promise to cancer patients.
Worldwide, a number of research groups are functioning towards effective treatment of colon cancer using chemotherapeutic agents. Nonsteroidal anti-inflammatory drugs are among the most potent agents discovered for the inhibition of cancer. In spite of the approval of celecoxib for adjuvant therapy in patients with familial adenomatous polyposis and precancerous disease of colon, associations of larger intensity of side effects limit its usage in cancer therapy. Combination therapy provides advantages of reduction in dose and possible reduction in toxicity and acquired drug resistance. As a consequence, targeted drug delivery and targeted molecular therapy of single or combination of anticancer agents are necessary for efficient treatment of colon cancer with reduced toxicity. In our study, combination of celecoxib and AEE788 shows growth inhibition and apoptosis in HCT 15 cells. Further, nanocarrier mediated celecoxib delivery showed high entrapment efficiency, sustained release patterns, desirable hemocompatibility and enhanced cytotoxicity and apoptosis in vitro and in vivo.
A new Schiff base ligand (HL) derived from the condensation of quinoline-2-carboxaldehyde with 2-aminophenol and its mixed ligand complexes of Cr(III), Mn(II), Fe(III), Co(II), Ni(II), Cu(II), Zn(II) and Cd(II) vis 2,2'-bipyridine/1,10-phenanthroline as secondary ligand have been synthesized and characterized by elemental analyses, spectroscopic studies (IR, mass spectra, 1H NMR, UV-vis, magnetic susceptibility and solid reflectance), molar conductance, x-ray diffraction, ESR and thermal studies. The kinetic and thermodynamic parameters were calculated using the Coats-Redfern and HorowitzMetzger methods. Also, Schiff base ligand and its mixed ligand complexes were screened against Gram positive bacteria (Streptococcus pneumoniae and Bacillis subtilis) and Gram negative bacteria (Pseudomonas aeruginosa and Escherichia coli). Antifungal activity was carried out against (Aspergillus fumigatus and Candida albicans). In addition, anti-cancer activity of Schiff base ligand and its mixed ligand complexes were also tested against breast cancer cell line (MCF-7) and colon cancer cell line (HCT-116).
Synthesis, Characterization, Anti-Proliferation, Benzimidazole Derivatives, FTIR, HRMS, 1D, 2D NMR spectroscopy, X ray crystallography, benzylation, addition/elimination, cyclization reactions, o- vanillin, o-, m-, p-phenylenediamines, 2-benzyloxy-3- methoxybenzaldehyde, 2-amino-N-benzylidene benzeneamines, bis-Schiff bases, six , five membered illusory rings, tetrahedral mechanism or addition/elimination mechanism, breast cancer cell line MCF 7, colon cancer cell line HCT 116, MTT assay, cytotoxicity, and IC50.
The original work of the present book consists of three research projects: In the first part: Synthesis, cytotoxicity evaluation, molecular docking and utility of novel chalcones as precursors for heterocycles incorporating pyrazole moiety.In the second part: Synthesis and antimicrobial activity of novel azolopyrimidines and pyrido-triazolo-pyrimidinones incorporating pyrazole moiety.In the third part: Synthesis of new pyrazolyl-pyridines as antitumor agents. The assigned structures for all the newly synthesized compounds were confirmed on the basis of elemental analyses and spectral data and the mechanisms of their formation were also discussed. In addition, some of the newly synthesized chalcones were tested for their cytotoxicity against human colon carcinoma cell line (HCT-116) and against human hepatocellular carcinoma (HEPG2) cell lines and the results revealed that some compounds have promising activities compared with the standard drug Doxorubicin. Molecular docking was also carried out for the high potent compounds.
This work has been carried out to investigate the following: The first project represents the reactions of ethylidenethiosemicarbazone with DMAD or substituted methylenemalononitriles gave thiazolidin-4-one or 1,3-thiazine derivatives, respectively. Also, treatment of ethylidenethiosemicarbazide with hydrazonoyl halides, -haloketones, and chloroacetic acid afforded the corresponding arylazothiazoles, thiazoles, and thiazolidenone derivative, respectively. The anti-cancer activity of the selected products against the colon carcinoma cell line (HCT-116) was determined and the results revealed promising activity.The second project involves the synthesis of a novel series of pyridine and bipyridine derivatives is described via one-pot multi-component reaction of 5-acetylimidazole, malononitrile (or ethyl cyanoacetate or diethyl malonate), substituted benzaldehyde (or terephthaldehyde) and ammonium acetate in good yields. The antimicrobial activities of the synthesized compounds were screened and the results showed that most of them exhibit considerable activities. Also, some of the newly synthesized compounds were screened for their anticancer activity against two cell lines.