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  • br Synthetic strategies A plenty

    2018-10-22


    Synthetic strategies A plenty of synthetic methods have been outlined for the synthesis of pyrazolo[1,5-a]pyrimidines in the following section. Aminopyrazole-I has been used in a number of reactions to attain the synthesis of desired compounds through different routes as following:
    Anticancer activity
    Anti-proliferative agents The tumor suppressor gene p53 is a multifunctional protein responsible for maintaining genomic integrity and its mutation is known to cause tumors in humans [46]. P53 gene activates signaling for DNA repair initially, and when failure of DNA repair occurs, induces apoptosis or resperidone arrest [103]. As a downstream effectors of p53, after anti-mitogenic signals or DNA damage, p21 (cell-cycle inhibitor) bind to cyclin–CDK complexes to inhibit their catalytic activity and induce cell-cycle arrest [104]. Distraction of this checkpoint through deletion of the p21 protein, results in cell arrest failure in response to DNA damage, endoreduplication, and ultimately, apoptosis [105]. In 2005, A. Gopalsamy et al. [105] introduce a novel series of p21 chemoselective agents (33,34) with a pyrazolo[1,5-a]pyrimidin-7-yl phenyl amides nucleus were recognized via high throughput screening which had an IC50 of 0.4 μM in a p21 deficient cell line (80S14) an IC50 of 12 μM in a p21 proficient cell line (HCT116), human colon carcinoma cell, with a selectivity index of 30 (ratio of IC50s of p21-proficient and p21-deficient cells) (Table 8). SAR of the lipophilic region of the molecule illustrates a small branched aliphatic group as isopropyl or isobutyryl group was found to be perfect to achieve both potency and selectivity. From the linkers explored, carbamate and urea linkers were slightly more potent than an amide linker. The isopropyl carbamate derivative 34 was identified as a highly chemoselective agent displaying a potency of 51 nM in the p21 deficient cell line.
    Conclusion
    Introduction Mimosa pigra Linn (commonly known as giant sensitive plant, bashplant, catclaw mimosa or black mimosa) belongs to the sub-family Mimosoideae, in the lager family Fabaceae of legumes (Leguminosae). It is native to tropical America, and naturalised in tropical Asia, south-eastern USA, northern America, tropical Africa and many other warm oceanic islands. M. pigra L. grows abundantly in floodplains, swamps, shallow dams, dried river beds and riparian zones; and is economically important in folk medicine, as a green manure for poles, hedges and for fuel wood. M. pigra L. reproduces primarily by prolific seed production, and vegetative through cut stems. The shrub is distinguished from its closely related species Mimosa pudica (sensitive plant) by its large size, large pods and leaves, which have 6 to 16 pairs of pinnae as opposed to 1 to 2 pairs in M. pudica leaves [1]. M. pigra L. has been described as an environmental invasive weed in several parts of the world and often threatens biodiversity. It is listed among 100 of the “World\'s Worst” invading plants by the IUCN Invasive Species Specialist Group. It is also included in the USA Federal Noxious Weeds List and has been listed as a noxious weed in Australia. In South Africa, M. pigra L. was identified as a Category 3 invader; thus no further propagation of the plant is allowed by state law, except with special permission and the existing plants are vehemently prevented from spreading. Sonibare and Gbile [2] reported the use of M. pigra L. in traditional medicine for the treatment of asthma and other respiratory diseases. Among the Bawku people in Upper East Ghana, the herb is used in the treatment of diarrhoea, typhoid fever and genitourinary tract infections [3]. The resperidone roots of M. pigra L. are sniffed for head colds, while a decoction of the leafy stem is used as a mouthwash for toothaches, and the fruits are used in eye medicines [4]. It is also used for the treatment of snakebite in Africa [5]. In Mexico, an infusion of M. pigra L. was traditionally used in Mayan medicine for treatment of diarrhoea [6]. While in Sumatra, the roasted and ground M. pigra L. leaves are made into an infusion, and drunk to treat a weak heart or weak pulse [7]. The pronounced usage of M. pigra L. in the folk medicinal systems of Bangladesh to lower blood sugar in diabetic patients and for the treatment of pain prompted Ahmed et al. [8] to investigate and confirm the antidiabetic and antinociceptive effects of M. pira L.