Day: December 3, 2021

An article Discovery of Potent and Selective Non-Nucleotide Small Molecule Inhibitors of CD73 WOS:000529170200009 published article about ECTO-5′-NUCLEOTIDASE; INSIGHTS; 5-NUCLEOTIDASE; EXPRESSION; ANTI-CD73; ADENOSINE; THERAPY; CD39 in [Beatty, Joel W.; Lindsey, Erick A.; Thomas-Tran, Rhiannon; Debien, Laurent; Mandal, Debashis; Jeffrey, Jenna L.; Tran, Anh T.; Fournier, Jeremy; Jacob, Steven D.; Yan, Xuelei; Drew, Samuel L.; Ginn, Elaine; Chen, Ada; Pham, Amber T.; Zhao, Sharon; Jin, Lixia; Young, Stephen W.; Walker, Nigel P.; Leleti, Manmohan Reddy; Powers, Jay P.; Lawson, Kenneth, V] Arcus Biosci Inc, Hayward, CA 94545 USA; [Moschuetz, Susanne; Straeter, Norbert] Univ Leipzig, Ctr Biotechnol & Biomed, Inst Bioanalyt Chem, D-04103 Leipzig, Germany in 2020.0, Cited 32.0. Safety of 3-Hydroxybenzaldehyde. The Name is 3-Hydroxybenzaldehyde. Through research, I have a further understanding and discovery of 100-83-4

CD73 is an extracellular mediator of purinergic signaling. When upregulated in the tumor microenvironment, CD73 has been implicated in the inhibition of immune function through overproduction of adenosine. Traditional efforts to inhibit CD73 have involved antibody therapy or the development of small molecules, the most potent of which mimic the acidic and ionizable structure of the enzyme’s natural substrate, adenosine 5′-monophosphate (AMP). Here, we report the systematic discovery of a novel class of non-nucleotide CD73 inhibitors that are more potent than all other nonphosphonate inhibitor classes reported to date. These efforts have culminated in the discovery of 4(-{5-[4-fluoro-1-(2H-indazol-6-yl)-1H-1,2,3-benzotriazol-6-yl]-1H-pyrazol-1-yl}methyl)benzonitrile (73, IC50 = 12 nM) and 4-({5[4-4-chloro-1-(2H-indazol-6-yl)-1H-1,2,3-benzotriazol-6-yl]-1H-pyrazol-1-yl}methyl)benzonitrile (74, IC50 = 19 nM). Cocrystallization of 74 with human CD73 demonstrates a competitive binding mode. These compounds show promise for the improvement of drug-like character via the attenuation of the acidity and low membrane permeability inherent to known nucleoside inhibitors of CD73.

Welcome to talk about 100-83-4, If you have any questions, you can contact Beatty, JW; Lindsey, EA; Thomas-Tran, R; Debien, L; Mandal, D; Jeffrey, JL; Tran, AT; Fournier, J; Jacob, SD; Yan, XL; Drew, SL; Ginn, E; Chen, A; Pham, AT; Zhao, SR; Jin, LX; Young, SW; Walker, NP; Leleti, MR; Moschutz, S; Strater, N; Powers, JP; Lawson, KV or send Email.. Safety of 3-Hydroxybenzaldehyde

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Name: Mequinol. In 2021.0 DRUG METAB PHARMACOK published article about CATALYTIC-PROPERTIES; HYDROLYSIS; ISOZYMES; AGENT in [Takahashi, Masato; Hirota, Ibuki; Nakano, Tomoyuki; Kotani, Tomoyuki; Takani, Daisuke; Shiratori, Kana; Choi, Yura; Haba, Masami; Hosokawa, Masakiyo] Chiba Inst Sci, Fac Pharm, 15-8 Shiomi Cho, Choshi, Chiba 2880025, Japan in 2021.0, Cited 25.0. The Name is Mequinol. Through research, I have a further understanding and discovery of 150-76-5.

Carboxylesterase (CES) plays an important role in the hydrolysis metabolism of ester-type drugs and prodrugs. In this study, we investigated the change in the hydrolysis rate of hCE1 by focusing on the steric hindrance of the ester structure and the electron density. For 26 kinds of synthesized indomethacin prodrugs, the hydrolytic rate was measured in the presence of human liver microsomes (HLM), human small intestine microsomes (HIM), hCE1 and hCE2. The synthesized prodrugs were classified into three types: an alkyl ester type that is specifically metabolized by hCE1, a phenyl ester type that is more easily metabolized by hCE1 than by hCE2, and a carbonate ester type that is easily metabolized by both hCE1 and hCE2. The hydrolytic rate of 1-methylpentyl (hexan-2-yl) ester was 10-times lower than that of 4-methylpentyl ester in hCE1 solution. hCE2 was susceptible to electron density of the substrate, and there was a difference in the hydrolysis rate of up to 3.5-times between p-bromophenyl ester and p-acetylphenyl ester. By changing the steric hindrance and electron density of the alkoxy group, the factors that change the hydrolysis rate by CES were elucidated. (C) 2021 The Japanese Society for the Study of Xenobiotics. Published by Elsevier Ltd. All rights reserved.

Welcome to talk about 150-76-5, If you have any questions, you can contact Takahashi, M; Hirota, I; Nakano, T; Kotani, T; Takani, D; Shiratori, K; Choi, Y; Haba, M; Hosokawa, M or send Email.. Name: Mequinol

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Safety of 3,4-Dimethoxybenzaldehyde. Authors Abosalim, HM; Nael, MA; El-Moselhy, TF in WILEY-V C H VERLAG GMBH published article about in [Abosalim, Heba M.; Nael, Manal A.; El-Moselhy, Tarek F.] Tanta Univ, Fac Pharm, Dept Pharmaceut Chem, Tanta 31527, Egypt in 2021.0, Cited 31.0. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9

Twenty derivatives of chalcones were synthesized and their anticancer activities were estimated against both breast and liver cancer besides two human normal cell lines. Out of our candidates, there were five compounds 3 b, 3 d, 3 h, 7 and 10 b that revealed a broad superlative antitumor activity against both HepG2 and MCF7 cell lines. Surprisingly, 3 h showed the most powerful anticancer activity (GI(50)=5.43 +/- 0.170 mu M for MCF7 and GI(50)=1.80 +/- 0.50 mu M for HepG2) and displayed the most effective inhibition activity on tubulin with IC50=4.51 +/- 0.13 mu M. 3 h exerted low toxicity toward both normal human, Hs371.T and AML12, cell lines. 3 h revealed arrest of cell cycle at G2/M and induced apoptosis compared to control cells. Docking study of all newly derivatives was achieved to decide the preeminent binding mode. Generally, the outcome of the docking study showed that 3 h had better binding mode.

Safety of 3,4-Dimethoxybenzaldehyde. Welcome to talk about 120-14-9, If you have any questions, you can contact Abosalim, HM; Nael, MA; El-Moselhy, TF or send Email.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Product Details of 123-11-5. In 2021 NAT PROD RES published article about (+)-USNIC ACID in [Van-Kieu Nguyen; Chavasiri, Warinthorn] Chulalongkorn Univ, Fac Sci, Ctr Excellence Nat Prod Chem, Dept Chem, Bangkok, Thailand; [Sichaem, Jirapast] Thammasat Univ, Fac Sci & Technol, Lampang Campus, Lampang, Thailand; [Huu-Hung Nguyen; Thi-Phuong Nguyen] Nguyen Tat Thanh Univ, Fac Biotechnol & Environm, Ho Chi Minh City, Vietnam; [Xuan Hieu Nguyen; Thi-Thu-Loi Huynh; Duc-Dung Pham] Ho Chi Minh City Univ Educ, Dept Chem, Ho Chi Minh City, Vietnam; [Niamnont, Nakorn] King Mongkuts Univ Technol Thonburi, Fac Sci, Dept Chem, Organ Synth Electrochem & Nat Prod Res Unit, Bangkok, Thailand; [Dinh-Hung Mac] Ha Noi Natl Univ, Univ Sci, Dept Organ Chem, Hanoi, Vietnam; [Kim-Phi-Phung Nguyen] Natl Univ Ho Chi Minh City, Univ Sci, Dept Organ Chem, Ho Chi Minh City, Vietnam; [Thuc-Huy Duong] Ton Duc Thang Univ, Dept Management Sci & Technol Dev, Ho Chi Minh City, Vietnam; [Thuc-Huy Duong] Ton Duc Thang Univ, Fac Appl Sci, Ho Chi Minh City, Vietnam in 2021, Cited 13. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5.

A series of usnic acid benzylidene derivatives (groups I-V) were designed, synthesized and evaluated for their anticancer activity in the search for potentially new anticancer agents. Compounds 1a, 5b, 2b, 2e and 2f exhibited the most potent cytotoxcity against K562 cell line with IC50 values of 10.0 +/- 3.6, 5.6 +/- 0.4, 8.8 +/- 1.0, 4.5 +/- 0.1 and 8.4 +/- 0.4 mu M, respectively. It is noteworthy that compound 2e displayed potent cytotoxicity against K562 cells without any cytotoxic effect on HEK293 normal cell line.

Product Details of 123-11-5. Bye, fridends, I hope you can learn more about C8H8O2, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

An article Nickel-Catalyzed ortho-Acyloxylation of Benzamides and Acrylamides with Carboxylic Acids WOS:000513245800016 published article about C-H BONDS; UNACTIVATED C(SP(3))-H BONDS; DIRECT THIOLATION; C(SP(2))-H BONDS; ALIPHATIC AMIDES; DIRECT ARYLATION; CARBON; FUNCTIONALIZATION; BENZOXYLATION; ACETOXYLATION in [Lin, Jingyi; Guo, Zhao; Lin, Cong; Gao, Fei; Shen, Liang] Jiangxi Sci & Technol Normal Univ, Coll Chem & Chem Engn, Jiangxi Engn Lab Waterborne Coatings, Nanchang 330013, Jiangxi, Peoples R China in 2020, Cited 63. COA of Formula: C5H8O2. The Name is (E)-2-Methylbut-2-enoic acid. Through research, I have a further understanding and discovery of 80-59-1

The nickel-catalyzed ortho-acyloxylation of C(sp(2))-H bonds of benzamides and acrylamides assisted by8-aminoquinolyl auxiliary has been realized for the first time. A wide range of carboxylic acids were compatible in this protocol to provide diverse carboxylic esters in moderate to excellent yields.

Welcome to talk about 80-59-1, If you have any questions, you can contact Lin, JY; Guo, Z; Lin, C; Gao, F; Shen, L or send Email.. COA of Formula: C5H8O2

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

An article Hydroxyl substituted benzoic acid/cinnamic acid derivatives: Tyrosinase inhibitory kinetics, anti-melanogenic activity and molecular docking studies WOS:000499694600003 published article about VANILLIC ACID; CINNAMIC ACID; L-DOPA; MUSHROOM; MECHANISM; ANTIOXIDANT; PROLIFERATION; PIGMENTATION; ANALOGS in [Nazir, Yasir; Zuegg, Johannes; Cooper, Matthew A.; Blaskovich, Mark A. T.; Ziora, Zyta M.] Univ Queensland, Inst Mol Biosci, St Lucia, Qld 4072, Australia; [Nazir, Yasir; Ashraf, Zaman] Allama Iqbal Open Univ, Dept Chem, Islamabad 44000, Pakistan; [Saeed, Aamer] Quaid i Azam Univ, Dept Chem, Islamabad 45320, Pakistan; [Rafiq, Muhammad] Cholistan Univ Vet & Anim Sci, Dept Physiol & Biochem, Bahawalpur, Pakistan; [Afzal, Samina] Bahauddin Zakria Univ, Fac Pharm, Multan 60800, Pakistan; [Ali, Anser] Mirpur Univ Sci & Technol, Dept Zool, Mirpur 10250, Ajk, Pakistan; [Latif, Muhammad] Taibah Univ, Coll Med, CGID, Al Madinah Al Munawwarah, Saudi Arabia; [Hussein, Waleed M.; Barnard, Ross T.] Univ Queensland, SCMB, St Lucia, Qld 4072, Australia; [Hussein, Waleed M.; Barnard, Ross T.] Univ Queensland, ARC Training Ctr Biopharmaceut Innovat, St Lucia, Qld 4072, Australia; [Hussein, Waleed M.] Helwan Univ, Fac Pharm, Pharmaceut Organ Chem Dept, Einhelwan, Helwan, Egypt; [Fercher, Christian] Univ Queensland, Australian Inst Bioengn & Nanotechnol, St Lucia, Qld 4072, Australia in 2020.0, Cited 47.0. The Name is m-Methoxyphenol. Through research, I have a further understanding and discovery of 150-19-6. Recommanded Product: 150-19-6

The inhibition of tyrosinase is an established strategy for treating hyperpigmentation. Our previous findings demonstrated that cinnamic acid and benzoic acid scaffolds can be effective tyrosinase inhibitors with low toxicity. The hydroxyl substituted benzoic and cinnamic acid moieties of these precursors were incorporated into new chemotypes that displayed in vitro inhibitory effect against mushroom tyrosinase. The most active compound, (2-(3-methoxyphenoxy)-2-oxoethyl (E)-3-(4-hydroxyphenyl) acrylate) 6c, inhibited tyrosinase with an IC50 of 5.7 mu M, while (2-(3-methoxyphenoxy)-2-oxoethyl 2, 4-dihydroxybenzoate) 4d had an IC50 of 23.8 mu M. In comparison, the positive control, kojic acid showed tyrosinase inhibition with an IC50 = 16.7 mu M. Analysis of enzyme kinetics revealed that 6c and 4d displayed noncompetitive reversible inhibition of the second tyrosinase enzymatic reaction with K-i values of 11 mu M and 130 mu M respectively. In silico docking studies with mushroom tyrosinase (PDB ID 2Y9X) predicted possible binding modes in the catalytic site for these active compounds. The phenolic para-hydroxy group of the most active compound 6c is predicted to interact with the catalytic site Cu++ ion. The methoxy part of this compound is predicted to form a hydrogen bond with Arg 268. Compound 6c had no observable toxic effects on cell morphology or cell viability at the highest tested concentration of 91.4 mu M. When dosed at 91.4 mu M onto B16F10 melanoma cells in vitro 6c showed anti-melanogenic effects equivalent to kojic acid at 880 mu M. 6c displayed no PAINS (pan-assay interference compounds) alerts. Our results show that compound 6c is a more potent tyrosinase inhibitor than kojic acid and is a candidate for further development. Our exposition of the details of the interactions between 6c and the catalytic pocket of tyrosinase provides a basis for rational design of additional potent inhibitors of tyrosinase, built on the cinnamic acid scaffold.

Recommanded Product: 150-19-6. Welcome to talk about 150-19-6, If you have any questions, you can contact Nazir, Y; Saeed, A; Rafiq, M; Afzal, S; Ali, A; Latif, M; Zuegg, J; Hussein, WM; Fercher, C; Barnard, RT; Cooper, MA; Blaskovich, MAT; Ashraf, Z; Ziora, ZM or send Email.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Recently I am researching about POLY(ARYLENE ETHER SULFONE); PROTON-EXCHANGE MEMBRANES; POLYMER ELECTROLYTE MEMBRANE; RANDOM STATISTICAL COPOLYMERS; BLOCKS, Saw an article supported by the Department of EnergyUnited States Department of Energy (DOE); Giner Inc. [DE-EE0000471]; National Science FoundationNational Science Foundation (NSF) [DMR-0923107, DMR-1126534]. SDS of cas: 150-76-5. Published in ELSEVIER SCI LTD in OXFORD ,Authors: Rowlett, JR; Shaver, AT; Mecham, S; Riffle, JS; McGrath, JE. The CAS is 150-76-5. Through research, I have a further understanding and discovery of Mequinol

A multiblock copolymer with increased charge density in the hydrophilic phase was synthesized by utilizing a trisulfonated poly(arylene ether sulfone) backbone (SHQS100). To achieve a balance of membrane properties a partially fluorinated poly(arylene ether benzonitrile) hydrophobic phase (6FPAEB) was used in uneven block lengths to form the hydrophilic-hydrophobic multiblock copolymer. Multiblock copolymers were synthesized via nucleophilic aromatic substitution to achieve high molecular weight copolymers and corresponding ductile membranes. Combination of the shorter increased charge density hydrophilic phase and longer partially fluorinated hydrophobic phase resulted in superior proton conductivity and mechanical properties while limiting water uptake and swelling, despite high ion-exchange capacity. The trifunctional SHQSH hydrophilic phase is proposed to produce a more concentrated charge region in the hydrophilic phase, while swelling of the membrane was limited by a longer partially fluorinated hydrophobic phase.

Welcome to talk about 150-76-5, If you have any questions, you can contact Rowlett, JR; Shaver, AT; Mecham, S; Riffle, JS; McGrath, JE or send Email.. SDS of cas: 150-76-5

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Sina, KF; Yahyazadeh, A; Mahmoodi, NO in [Sina, Kiana Faraji; Yahyazadeh, Asieh; Mahmoodi, Nosrat Ollah] Univ Guilan, Fac Sci, Dept Chem, POB 41335-1914, Rasht, Iran published Synthesis, Characterization and Antibacterial Evaluation of 2, 3Dihydroquinazolin-4 (1H)-Ones and Some New Bis 2, 3-Dihydroquinazolin-4 (1H)-Ones Using Pre-made Pyrazole Carbaldehyde Derivatives in 2021, Cited 41. Product Details of 99-93-4. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4.

2, 3-Dihydroquinazolinones are of popular compounds with the diversification of biological and pharmacological activities. Among many discovered methods, there are efficient and convenient methods used for the synthesis of 2, 3-dihydroquinazoline-4 (1H)-one and some new bis 2, 3-dihydroquinazoline-4 (1H)-one derivatives which are reported in this study. The mentioned methods include the two-component condensation of one molecule of anthranilamide and one molecule of pyrazole carbaldehyde using montmorillonite-K 10 as a catalyst for the preparation of 2, 3 dihydroquinazoline-4 (1H)-ones. Also, one-pot pseudo-five-component reaction (5MCRs) of two molecules of isatoic anhydride, two molecules of pyrazole carbaldehydes and one molecule of ethan-1, 2-diamine in the presence of the r catalyst (montmorillonite-K10) for the synthesis of bis 2, 3-dihydroquinazoline-4 (1H)-ones. Despite the short times of reactions, high yields of products were obtained, which were validated using FT-IR, (HNMR)-H-1, (CNMR)-C-13, and elemental analysis. Moreover, the compounds were screened for their antimicrobial activities against two-gram-positive bacterial strains: Staphylococcus aureus and Micrococcus Luteus; and against two-gram-negative bacterial strains, as well: Escherichia coli and Pseudomonas aeruginosa, which all were utilized for antibacterial investigations. The results showed moderate or significant antibacterial activities.

Product Details of 99-93-4. Welcome to talk about 99-93-4, If you have any questions, you can contact Sina, KF; Yahyazadeh, A; Mahmoodi, NO or send Email.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Product Details of 98-17-9. In 2019 ORG LETT published article about C-C; INTRAMOLECULAR HYDROALKOXYLATION; INTERMOLECULAR HYDROALKOXYLATION; HIGHLY EFFICIENT; ALKYNES; HYDROAMINATION; COMPLEXES; TRANSFORMATION; CYCLOISOMERIZATION; ACETALS in [Laserna, Victor; Rojas, Catherine Jeapes; Sheppard, Tom D.] UCL, Dept Chem, 20 Gordon St, London WC1H 0AJ, England in 2019, Cited 43. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9.

A practical method for the synthesis of phenyl enol ethers is reported. The combination of a gold(I) catalyst and potassium carbonate selectively mediates the addition of phenols to propargylic alcohols/amines in a chemo-, regio-, and stereoselective fashion in high yield. The resulting enol ethers are formed exclusively with a Z-configuration and can be obtained from a wide array of phenols and propargylic alcohols or amines with the reaction showing excellent functional group tolerance.

Bye, fridends, I hope you can learn more about C7H5F3O, If you have any questions, you can browse other blog as well. See you lster.. Product Details of 98-17-9

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

An article Novel prenyloxy chalcones as potential leishmanicidal and trypanocidal agents: Design, synthesis and evaluation WOS:000461728400027 published article about DERIVATIVES; PREVENTION; DISEASE in [Espinoza-Hicks, Jose C.; Hernandez-Rivera, Jessica L.; Camacho-Davila, Alejandro] Univ Autonoma Chihuahua, Fac Ciencias Quim, Campus Univ,Apartado Postal 669, Chihuahua, Chih, Mexico; [Fabiola Chacon-Vargas, Karla; Enid Sanchez-Torres, Luvia] Inst Politecn Nacl, Escuela Nacl Ciencias Biol, Dept Inmunol, Prolongac Carpio & Plan de Ayala S-N, Mexico City 11340, DF, Mexico; [Fabiola Chacon-Vargas, Karla; Nogueda-Torres, Benjamin] Inst Politecn Nacl, Escuela Nacl Ciencias Biol, Dept Parasitol, Prolongac Carpio & Plan de Ayala S-N, Mexico City 11340, DF, Mexico; [Tamariz, Joaquin] Inst Politecn Nacl, Escuela Nacl Ciencias Biol, Dept Quim Organ, Prolongac Carpio & Plan de Ayala S-N, Mexico City 11340, DF, Mexico in 2019.0, Cited 43.0. Category: indole-building-block. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4

The available drugs for treating Leishmaniasis and American trypanosomiasis have high toxicity and multiple side effects, among other problems. More effective and less toxic treatments are urgently needed. A series of chalcones that contained a prenyloxy or geranyloxy substituent was synthesized and characterized. Each substituent was attached to the A ring in some compounds and to the B ring in others, with additional substituents placed on the chalcone moiety. The present aim was to evaluate the effect of the substitution pattern on leishmanicidal and trypanocidal activity. When tested at a single concentration, the compounds exerting a metabolic inhibition close to or exceeding 50% for Leishmania mexicana were 11, 17 and 12, and for Trypanosoma cruzi were 11, 17, 15 and 26. Upon determining the selectivity index (SI =IC50/CC50), the values were 80.9, 1.24 and 55.12 for 11, 17 and 12 (respectively) versus L mexicana, and 75.1, 1.43, 27.36 and 33.52 for 11, 17, 15 and 26 (respectively) versus T. cruzi. Structural isomers 11 and 17 showed activity for both the L mexicana and T. cruzi strains, though the greater cytotoxic activity of 17 led to a lower SI. Compounds 12, 15 and 26 were species specific. For I cruzi, the SI was higher for 11, 15 and 26 than for the reference drugs nifurtimox and benznidazole. The examination of promastigote morphology after exposing L mexicana and T. cruzi to 11 revealed a decrease in cell density. The current findings suggest that 11 could be a useful lead compound for further SAR studies. (C) 2019 Elsevier Masson SAS. All rights reserved.

Category: indole-building-block. Welcome to talk about 99-93-4, If you have any questions, you can contact Espinoza-Hicks, JC; Chacon-Vargas, KF; Hernandez-Rivera, JL; Nogueda-Torres, B; Tamariz, J; Sanchez-Torres, LE; Camacho-Davila, A or send Email.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles