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As pyrazole and isoxazole based derivatives are well-known for displaying a considerable biological profile, an attempt has been made to unravel their cytotoxic potential. In this context, a number of pyrazole/isoxazole linked arylcinnamide conjugates (15a-o and 21a-n) have been synthesized by employing a straight forward route. The basic structure comprised three ring scaffolds (A, B and C): methoxyphenyl rings as A and C rings and a five membered heterocyclic ring (pyrazole or isoxazole) as the B-ring. To achieve clear understanding, these derivatives are categorized as pyrazole-phenylcinnamides (PP) and isoxazole-phenylcinnamides (IP). These compounds have been evaluated for their ability to inhibit the growth of various human cancer cell lines such as HeLa, DU-145, A549 and MDA-MB231 and most of them exhibit considerable cytotoxic effects. Some of them like 15a, 15b, 15e, 15i and 15l exhibit promising cytotoxicity in HeLa cells (IC50 = 0.4, 1.8, 1.2, 2.7 and 1.7 μM). Amongst them 15a, 15b and 15e were taken up for detailed biological studies, they were found to arrest the cells in the G2/M phase of the cell cycle. Moreover, they were investigated for their effect on the microtubular cytoskeletal system by using a tubulin polymerization assay, immunofluroscence and molecular docking studies; interestingly they demonstrate a significant inhibition of tubulin polymerization.

Linum usitatissimum commonly known as flax or linseed is an important medicinal plant, produces medicinally potent lignans, used in the treatment of several human diseases. Lignans limited production in the natural plants does not meet the increasing market demand. This study was conducted to establish an easy and rapid method for the in vitro micropropagation and production of potent lignans and antioxidant secondary metabolites in linseed. The results indicated that hypocotyl explants under the effects of thidiazuron (TDZ: 0.5 mg/L) + kinetin (Kn: 0.5 mg/L) in the basal growth media, resulted in the optimal shoot organogenesis parameters (shoot induction frequency: 86.87%, number of shoots: 6.3 ± 0.36 and shoots length: 6.5 ± 0.54 cm), in 4 weeks. Further, TDZ supplementation in the culture media efficiently activated the antioxidant system in the in vitro raised shoots, wherein maximum production of total phenolic content, TPC (34.33 ± 0.20 mg of GAE/g DW); total flavonoid content, TFC (8.99 ± 0.02 mg of QE/g DW); DPPH free radical scavenging activity (92.7 ± 1.32%); phenylalanine ammonia-lyase activity, PAL (8.99 ± 0.02 U/g FW); and superoxide dismutase expression, SOD (3.62 ± 0.01 nM/min/mg FW) were observed in the shoot cultures raised in presence of TDZ: 0.5 mg/L + Kn: 0.5 mg/L. Nonetheless, considerable levels of pharmacologically active lignans such as secoisolariciresinol (SECO: 23.13–37.10 mg/g DW), secoisolariciresinol diglucoside (SDG: 3.32–3.86 mg/g DW) and anhydrosecoisolariciresinol diglucoside (ANHSECO: 5.15–7.94 mg/g DW) were accumulated in the regenerated shoots. This protocol can be scaled up for the commercial production of linseed to meet the market demands for lignans.

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The efficacy of methanolic seed extracts of Amomum subulatum Roxb. activity against bacterias such Staphylococcus aureus, Streptococcus pneumoniae, Bacillus subtilis, Salmonella typhi, Klebsiella pneumoniae, Pseudomonas aerugenosa and Candida albican senegalensis was studied. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of the extracts was determined using standard methods. Results obtained showed considerable inhibition against the bacteria tested except Salmonella pyrogenes and Escheria Coli which showed considerable resistance at all concentrations of the extract. It can also observe that the extract exhibited greater inhibition on Klebsiella pneumonia and Pseudomonas aerugenosa (18±0.2 and 17±0.3). However the standard antibacterial drug tetracycline exhibit superior activity than the extract. Both the MICs and MBCs of the extract ranges from 50 to 200 mg/ml. Its further reveals that Bacillus subtilis, Klebsiella pneumonia and Staphylococcus aureus exhibit broadest activity at MIC and MBC concentrations of 50mg/ml. While the rest Salmonella typhii and Pseudomonas aerogunosa and candida albicans of the bacteria shows negative turbidity and resistance at MIC and MBC of 100mg/ml. This activity was indicative of the possible means of finding pure active principles from natural source with possible high potency that could serve as a lead to the pharmaceuticals. The low concentration (MIC and MBC) activity of the methanolic extracts give credence and scientific base for the claim therapeutic capabilities of Amomum subulatum as an anti-bacterial agent. The extract concentrate yield of the methanolic extracts was estimated to be 9.8%w/w which is brown in colour and oily in texture. Preliminary screening analysis of the powdered methanolic seed extracts showed the presence of Carbohydrate, tannins, cardioactive glycosides, tepenes, flavonoids, alkaloids and saponins. Anthraquinone was not found in the extract. The study provides the basis of use of this plant Amomum subulam in treatment of infections caused by pathogens (bacteria) and the phytochemical found are implicated in having anti-bacterial properties.

Background: Imidazo[2,1-b]thiazole, a well known fused five membered hetrocycle, is one of the most promising and versatile moiety in the area of medicinal chemistry. Derivatives of imidazo[2,1-b]thiazole have been investigated for the development of new derivatives that exhibit diverse pharmacological activities. This fused heterocycle is also a part of a number of therapeutic agents. Objective: To review the extensive pharmacological activities of imidazo[2,1-b]thiazole derivatives and the new molecules developed between 2000-2018 and usefulness. Method: Thorough literature review of all relevant papers and patents was conducted. Conclusion: The present review, covering a number of aspects, is expected to provide useful insights towards the design of imidazo[2,1-b]thiazole based compounds and would inspire the medicinal chemists for a comprehensive and target oriented information to achieve a major breakthrough in the development of clinically viable candidates.

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