Religiosity and Associations with Substance Use and Delinquency Among Urban African American Adolescents.

Adolescent delinquency and substance use are global problems. African American adolescents are especially susceptible to the life-changing consequences of these problem behaviors. Religiosity is a notable protective factor that has been shown to mitigate these behaviors. This study uses a person-centered approach to examine the extent to which religiosity is associated with lower rates of delinquency and substance use among urban African American adolescents in the United States. Latent Class Analysis was used to examine the heterogeneity in five religiosity items among a sample of adolescents ages 13-18. After identifying religiosity classes through a class enumeration process, we examined predictors of the classes using multinomial logistic regression. The classes were then used to predict several substance use and delinquency outcomes. Three religiosity classes were identified; "low religious beliefs and engagement," (15.19%, n = 94), "religious with low active engagement," (56.70%, n = 351), and "religious with high active engagement," (28.11%, n = 174). Protective effects of religiosity on substance use (e.g., alcohol) and delinquency were found (e.g., assault). Implications for research and practice are discussed.

Controlled microwave-assisted reactions: A facile synthesis of polyfunctionally substituted phthalazines as dual EGFR and PI3K inhibitors in CNS SNB-75 cell line.

Brain tumors are stubborn cancers with poor prognosis and disappointing survival rates. Targeted cancer therapeutics with higher efficacy and lower resistance are highly demanded. An efficient one-pot synthesis of polyfunctionalized phthalazines derivatives was developed by reacting ethyl 1-aryl-5-cyano-1,6-dihydro-4-methyl-6-oxo-3-pyridazine-carboxylates with cinnamonitrile derivatives and the cycloaddition reaction of thieno[3,4-d]pyridazines with activated double or triple bond systems under controlled microwave heating with high yields. The resultant synthesized phthalazines (5a-e, 9 and 13) were tested for their in vitro anti-cancer activities by using in vitro one dose assay at National Cancer institute, USA. Only phthalazine (5b) showed broad spectrum anti-tumor activity against most tested cancer cell lines from all subpanels with mean % GI = 22.61. Interestingly, all tested compounds showed varying growth inhibitory activity against a particular cell line, CNS SNB-75 cell line, but (5b) exhibited the highest growth inhibitory activity against CNS-SNB-75 cell line with (GI% = 108.81) and (IC50 = 3.703 ± 0.2) compared to erlotinib; (IC50 = 12.5 ± 0.68). It caused Pre-G1 apoptosis and growth arrest at S phase. It also increased percentage of the total apoptotic cells in CNS-SNB-75 cell line (39.26%) compared to control cells (2.17%) in the annexin V-FITC experiment. It revealed pronounced EGFR inhibitory activity (IC50 = 47.27 ± 2.41 ng/mL) compared to erlotinib (IC50 = 30.7 ± 1.56 ng/mL). It also inhibited the different PI3K isoforms α, ß, γ and δ (with IC50 of 4.39, 13.6, 12.5 and 3.11 µg/mL, respectively compared to LY294002 (with IC50 of 12.7, 8.57, 6.89 and 5.7 µg/mL, respectively). It also caused significant lower protein expression levels of pPI3K, AKT, pAKT and Bcl2 and higher protein expression levels of BAX, Casp3 and Casp9 when compared to untreated cells. Conclusion: Phthalazine (5b) may be an effective, convenient and safe anti-cancer agent acting via proapoptotic and dual EGFR and PI3K kinase inhibitory actions in CNS SNB-75 cell line.

Microwave-assisted efficient one-pot synthesis of N 2-(tetrazol-5-yl)-6-aryl/heteroaryl-5,6-dihydro-1,3,5-triazine-2,4-diamines.

An efficient one-pot synthesis of N 2-(tetrazol-5-yl)-6-aryl/heteroaryl-1,3,5-triazine-2,4-diamine derivatives was developed by reacting 5-amino-1,2,3,4-tetrazole with aromatic aldehydes and cyanamide in pyridine under controlled microwave heating with high yields. X-ray crystallography confirmed the structure of the obtained products.

Densely functionalized cinnolines: Controlled microwave-assisted facile one-pot multi-component synthesis and in vitro anticancer activity via apoptosis induction.

There is an urging continuous need for novel anti-cancer agents due to persistent chemoresistance. Herein, newly synthesized cinnolines are evaluated for their possible anticancer activities and suggested mechanisms. In the current study, a simple and efficient synthesis of densely functionalized cinnolines has been developed that relied on multi-component reaction of ethyl 5-cyano-4-methyl-1-aryl-6-oxo-1,6-dihydropyridazine-3-carboxylates with aromatic aldehydes and nitromethane in dioxane/pipridine under controlled microwave heating. Selected cinnolines (4a-c, e, h, j-n, q-v) were tested for possible anticancer activity using in vitro one dose assay at National Cancer institute, USA. Only cinnoline 4b stood out as the most potent cinnoline derivative (mean GI%=26.33) with broad-spectrum antitumor activity against the most tested cancer cell lines from all subpanels. The target cinnoline 4b emerged as the most active derivative against both leukemia RPMI-8226 and melanoma LOX IMVI cell lines (GI% = 106.06 and 82.1) respectively, with IC50 values equal to 17.12 ± 1.31 and 12.32 ± 0.75 µg/mL, which are comparable to those of staurosporin; 24.97 ± 1.47 and 8.45 ± 0.42 µg/mL, respectively. Cinnoline 4b influenced cell cycle distribution causing pre-G1 apoptosis and cell growth arrest at G2/M phase. It also induced apoptosis in both cell lines as manifested by significant increase in the percent of annexin V-FITC positive apoptotic cells in leukemia RPMI-8226 cells (from 1.09% to 12.47%) and melanoma LOX IMVI (from 1.32% to 19.05%). In addition, it showed lower expression levels of anti-apoptotic Bcl-2 protein, and higher expression levels of pro-apoptotic proteins; Bax, p53, cytochrome c, caspases 3 and 9. CONCLUSION: Induction of mitochondrial intrinsic pathway of apoptosis is a possible mechanism by which cinnoline 4b may confer its anticancer activity.

Aroyl and acyl cyanides as orthogonal protecting groups or as building blocks for the synthesis of heterocycles.

α-Cyanoketones represent a synthetically attractive scaffold possessing bifunctional reactivity which enabled synthesis of a diversity of products. This involves reaction of nucleophiles with electrophilic carbonyl carbon performing an efficient and regioselective way to acylation reaction, cycloaddition of activated cyano function with dipolarophiles, metal-catalyzed cross-dehydrogenative coupling carbocyanation across C-C multiple bonds as well as hydrocyanation. This review provides the recent developments in the chemistry of α-cyanoketones which will be beneficial for researchers and scientists in such field.