The Biological and Analytical Applications of Calixarenes Function: Facts and Growth Trends | Chapter 10 | Current Research and Development in Chemistry Vol.1

For over two decades, research on the biological and analytical applications of calixarenes and their derivatives has been shown remarkable properties towards organic and bioorganic molecules. Applications in the field of analytical chemistry and biological activity, as well as the anticancer properties of various calixarenes, have been studied and reported by several research groups. Due to their superior geometrical shape, calix[n]arenes structures (with n = 4; 6 or 8) have a special function, moreover, when combined with functional groups, the calixarenes can dissolve well and the low toxicity of the cell and the ability to form stable complexes with metal ion, especially the ability to transport drugs, it is allowed to be applied in the analysis and development of biosensors in fields: Biotechnology and drug discovery calixarene derivatives. The applications of calixarenes and their derivatives are summarized in this review, and future development prospects will be discussed.

Author(s) Details
Dr. Tran Quang Hieu
 Saigon Technology University, Ho Chi Minh City, Vietnam.

Dr. Nguyen Van Son
Faculty of Chemical Engineering, Industrial University of Ho Chi Minh City, Vietnam

Dr. Tran Nguyen Minh An
Faculty of Chemical Engineering, Industrial University of Ho Chi Minh City , Vietnam

Le Van Tan
Faculty of Chemical Engineering, Industrial University of Ho Chi Minh City, Vietnam

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Histo-Epidemiology of Kidney Cancer in Cameroon: About 110 Cases | Chapter 03 | New Insights into Disease and Pathogen Research Vol. 3

Objectives: To describe the epidemiological and histopathological aspects of kidney cancer in Cameroon.

Materials and Methods: This was a descriptive retrospective study on malignant tumors of the kidney examined in the anatomical pathology laboratories of five regions (Center, Littoral, West, South-west and North-west), over a period of 12 years (2004-2015). The studied parameters were: frequency, age, sex, histological type.

Results: A total of 110 cases of kidney cancer were collected, representing 8.55% of malignant urogenital tumors. The mean age of patients was 28.72±24.79 years (extremes: 4 months – 76 years). Females are relatively more affected than males (56 cases, 50.91%), with female-to-male ratio of 1.04:1. A total of 58 (52.73%) cases of renal cell carcinomas (RCC), 46 (41.82%) cases of nephroblastomas (NB) and 3 (2.73%) of soft tissue tumors were identified.

Conclusion: Kidney cancer is the third urogenital cancer in Cameroon characterized by a relative female predominance with renal cell carcinoma as the predominant histological type. Kidney cancer is the third urogenital cancer in Cameroon characterized by a relative female predominance with renal cell cancer as the predominant histological type. The fight against smoking, the prevention of diseases such as hypertension and diabetes are among the key elements that can help for the decrease in the prevalence of this pathology. It should be noted that the effective initiation of cancer registries is still essential to master the epidemiological data, foundation for a better coordination and prevention of the anti-cancer fight.

Author(s) Details

J. P. Ndamba Engbang
Faculty of Medicine and Pharmaceutical Sciences, The University of Douala, Douala, Cameroon.
Laquintinie Hospital of Douala, Douala, Cameroon.
North-Ossetian State Medical Academy, Vladikavkaz, Russia.

B. Sala
Faculty of Medicine and Pharmaceutical Sciences, The University of Douala, Douala, Cameroon.
Laquintinie Hospital of Douala, Douala, Cameroon.

C. Fonkwa
Laquintinie Hospital of Douala, Douala, Cameroon.

Y. Ligan
Faculty of Medicine and Pharmaceutical Sciences, The University of Douala, Douala, Cameroon.

B. Djougmo Djimeli
Laquintinie Hospital of Douala, Douala, Cameroon.

G. Simo
Bio-Medical and Cancer Center of Bafoussam, Bafoussam, Cameroon.

A. Moune
Anapathos Laboratory, Douala, Cameroon.

A. Fewou
Douala General Hospital, Douala, Cameroon.

J. L. Oyono Essame
Faculty of Medicine and Biomedical Sciences, The University of Yaoundé I, Yaoundé, Cameroon.
Yaounde University Health Center, Yaoundé, Cameroon.

A. Hasigov
North-Ossetian State Medical Academy, Vladikavkaz, Russia.

A. Ephiev
North-Ossetian State Medical Academy, Vladikavkaz, Russia.

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Novel Structures of Uracil Mustard (Uramustine) Retaining Cytotoxic Activity and Drug-likeness for Oral Administration | Chapter 16 | New Insights into Disease and Pathogen Research Vol. 2

Aims: To present 12 new variants of uracil mustard having drug-like properties and cytotoxic functional group, by utilizing uracil mustard (uramustine) as a lead compound. Utilize rigorous substructure and similarity of a molecular scaffold to determine drug like variants. Physicochemical properties determined indicate the variants have favorable drug-likeness.

Study Design: Conduct molecular database search utilizing features of substructure and similarity based upon uracil mustard.

Place and Duration of Study: Department of Chemistry, Medicinal Chemistry Study Section, University of Nebraska at Omaha, Omaha Nebraska between January 2015 to March 2015.

Methodology: Uracil mustard consists of the pyrimidine derivative uracil, having the bifunctional nitrogen mustard cytotoxic moiety covalently bonded onto the ring. A systematic search, utilizing substructure component and similarity, within an in-silico database search successfully determined 12 variants. Rigorous criteria for drug-likeness were implemented to screen potential candidates that included the application of the Rule of 5. In addition, maintaining the cytotoxic moiety of nitrogen mustard was crucial.

Results: A total of 12 variants of uracil mustard was identified after an extensive molecular database search using rigorous criteria. All 12 variants, and including uracil mustard, showed zero violations of the Rule of 5, thereby indicating favorable drug-likeness. Values of polar surface area for all compounds at less than 80 Angstroms2 are suitable for central nervous system penetration. Polar surface area, number of atoms, and Log P for all compounds increased as the molecular weight increases. Structure substituents include nitrogen mustard groups, hydroxyl, alkyl and carbonyl moieties. Cluster analysis discerned greatest similarity among members of this group.

Conclusion: Applying rigorous search criteria within a molecular data base, for comparison and reject, successfully identified 12 variants of uracil mustard that show favorable drug-likeness in addition to cytotoxic capability. The design of new antitumor agents is important for increasing efficacy of the clinical treatment of cancer. Variation of physicochemical properties can benefit the efficacy of anticancer drugs and should be further investigated for the benefit of patients.

Author(s) Details

Dr. Ronald Bartzatt
Durham Science Center, University of Nebraska, 6001 Dodge Street, Omaha, Nebraska 68182, USA.

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Measuring the Alkylation Kinetics and Drug Likeness of Four Novel Antineoplastic Compounds | Chapter 05 | Advances in Applied Science and Technology Vol. 4

Aims: To synthesize small molecule alkylating compounds and analyze the kinetics of the alkylation in aqueous solution. Determine molecular properties and the drug likeness of these four compounds as  potential  antineoplastic  agents  and  apply  statistical  analysis  to  identify  interrelationships  of properties.

Study  Design: Four  compounds  were  synthesized,  characterized,  and  studied  for  alkylation capability.  The  alkylation  kinetics was elucidated,  as  well  as  drug  likeness  properties.  The interrelationships of properties were examined by statistical methodology.

Place  and  Duration  of  Study: Department  of  Chemistry,  Durham  Science  Center,  University  of Nebraska at Omaha, Omaha NE, from May 2015 to June 2015.

Methodology: Four compounds were modified by the covalent bonding of an alkyl halide substituent or nitrogen mustard group. The four compounds were placed in aqueous solution at pH 7.4 and 37°C to  monitor  alkylation  efficiency  that  targeted  p-chloroaniline.  Alkylation  was  monitored  utilizing fluorescamine  and  measurement  at  400  nm.  Time  and  absorbance  plots  determined  whether alkylation step is first-order or second-order. Molecular properties Log P, formula weight, polar surface area, etc., were determined. Statistical analysis and path analysis revealed which molecular property was most responsible for rate constant values.

Results: Compounds A, B, C, and D showed ranges of Log P, formula weight, and polar surface area of  0.010  to  4.21,  177.59  to  714.77,  and  29.64  to  88.63,  respectively.  All  compounds  showed  a favorable drug likeness, with only compound C showing a violation of the Rule of 5. The Log P values and number of alkylation reactive sites were most responsible for rate constant value.

Conclusion: Small molecule alkylating agents are synthesized, the efficiency of alkylation measured in aqueous solution utilizing fluorescamine at pH 7.4 and 37°C. Rate-order of reactions is determined utilizing  fluorescamine  assay  for  surviving  primary  amine  groups.  The  four  compounds  showed  a favorable drug likeness based on molecular properties.

Author(s) Details

Dr. Ronald Bartzatt

University of Nebraska, Durham Science Center, 6001 Dodge Street, Omaha, Nebraska 68182, USA.

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View Volume: https://doi.org/10.9734/bpi/aast/v4